Selective defluorinative functionalization of trifluoromethylarenes(ArCF3)to obtain the pharmaceutically commonα,α-difluorobenzylic motif is an attractive and elegant synthetic route.Over the past decade,although C(...Selective defluorinative functionalization of trifluoromethylarenes(ArCF3)to obtain the pharmaceutically commonα,α-difluorobenzylic motif is an attractive and elegant synthetic route.Over the past decade,although C(sp^(3))-F bonds functionalization have been greatly developed,catalytic cross-coupling of trifluoromethylarenes with C-H of terminal alkynes remains a challenge.Here,we report an approach to achieve Sonogashira-type cross-coupling of trifluoromethylarenes with terminal alkynes C(sp)-H bonds via photoredox and Cu/L dual catalysis.Tridentate anionic ligand is pivotal to realize this C-H sp-sp^(3) cross-coupling.Moreover,this unique catalytic system is also suitable for cross-coupling of C(sp^(3))-F bonds with azoles C(sp^(2))-H bonds.A series of trifluoromethylarenes,terminal alkynes and azoles with various functional groups are compatible with this protocol affording a variety of defluoroalkynylation or defluoroazolation products.Preliminary mechanistic studies indicated that deprotonated BINOL involved as a photocatalyst to activate ArCF3 rather than a ligand to the metal.展开更多
The installation of azoles via C–H/N–H cross-coupling is significantly underdeveloped,particularly in benzylic C–H azolation due to the requirement for external chemical oxidants and the challenge in controlling th...The installation of azoles via C–H/N–H cross-coupling is significantly underdeveloped,particularly in benzylic C–H azolation due to the requirement for external chemical oxidants and the challenge in controlling the site-and chemo-selectivity.Herein,a late-stage azolation of benzylic C‒H bonds enabled by electrooxidation is described,which proceeds in an undivided cell under mild,catalyst-and chemical-oxidant-free reaction conditions.The strategy empowers the C‒H azolation on primary,secondary,and even challenging tertiary benzylic positions selectively.The remarkable synthetic utility of our approach is highlighted by its easy scalability without overoxidation of products and ample scope with valuable functional groups.The approach can be directly used to install benzyl and azole motifs on highly functionalized drug molecules.展开更多
Background: Vulvovaginal candidiasis (VVC) is a common cause of significant morbidity, affecting millions of women worldwide. It is estimated that approximately 75%of women of childbearing age will have at least one e...Background: Vulvovaginal candidiasis (VVC) is a common cause of significant morbidity, affecting millions of women worldwide. It is estimated that approximately 75%of women of childbearing age will have at least one episode of candidiasis in their lifetime. In the last decades, resistance to azoles has become a public health problem. Although studies on vulvovaginitis have been done, there is lack of VVC studies in our area. The aim of this study was to describe the etiological and resistance profiles of vulvovaginal candidiasis to standard antifungus at the Saint Camille Hospital of Ouagadougou (HOSCO), Burkina Faso. Methods: We conducted a prospective study from January 2018 to December 2022. From vulvovaginal swabs, Candida species were identified using the ChromID® Candida Agar medium and the API® Candida gallery. Antifungal susceptibility testing was performed using Kirby-Bauer agar disk diffusion. Results: A total of 4789 women were sampled. The average age of sexually active women was 27.80+/−6.77 years, with extremes ranging from 15 to 64 years. Vaginal Candida infections accounted for 74.16% of the cases. The 20 - 29 age group was the most affected by vulvovaginal candidiasis. Pregnant women accounted for 28.76% of our study population. Women in the second (2nd) trimester of pregnancy had more Candida infections. Candida albicans was the most isolated species (55.12%), followed by Candida glabrata (27.64%), Candida tropicalis (6.91%), Candida famata (6.67%), Candida krusei (2.56%). All the Candida species isolated showed very high of resistance to Fluconazole (45.2%), Miconazole (23.7%) and Clotrimazole (45.7%). Conclusion: Species-specific antifungal results should always be considered to avoid antifungal resistance associated with vulvovaginal candidiasis. Identifying the causative species using vaginal fungal cultures can help guide therapy and improve outcomes for these patients.展开更多
As an important chemical product,propylene(C_(3)H_(6))is widely used in production of many crucial chemical products such as polypropylene.Propane(C_(3)H_(8))is introduced as an inevitable gas impurity during the naph...As an important chemical product,propylene(C_(3)H_(6))is widely used in production of many crucial chemical products such as polypropylene.Propane(C_(3)H_(8))is introduced as an inevitable gas impurity during the naphtha cracking in propylene production.At present,thermal-driven energy-intensive cryogenic distillation is the most common purification method in industry.An energy-efficient,cost-effective and environmental-friendly separation technology is required to get polymer grade C_(3)H_(6)(higher than 99.5%).In face of the increasing demand of propylene,new separation technology based on porous adsorbents is expected to be a promising alternative.In recent years,metal-organic frameworks(MOFs)have obtained attention by their high porosity,regular adjustable pore shape and pore environment and keep making breakthroughs in separation and purification of many industrial gas mixtures,and are thus considered as one of the most potential types of adsorbents.The physical properties of C_(3)H_(6)and C_(3)H_(8),such as boiling point,size and kinetic diameter,are close to each other,making their separation a challenge.Most C_(3)H_(6)/C_(3)H_(8)sieving MOFs based on narrow sieving channels that restrict the access of molecules larger than their confined entrance purify mixtures at the cost of diffusion and capacity.To improve the adsorption of MOFs based on molecular sieving,a novel‘pearl-necklace’strategy was designed,which was named for its connected channel and molecular pocket vividly,but the diffusion limitation remains unsolved.展开更多
From the standpoint of chemical structures,the organic backbones of energetic materials can be classified into aromatic rings,nonaromatic rings,and open chains.Although the category of aromatic energetic compounds exh...From the standpoint of chemical structures,the organic backbones of energetic materials can be classified into aromatic rings,nonaromatic rings,and open chains.Although the category of aromatic energetic compounds exhibits several advantages in the regulation of energetic properties,the nonaromatic heterocycles,assembling nitramino explosophores with simple alkyl bridges,still have prevailed in benchmark materials.The methylene bridge plays a pivotal role in the constructions of the classic nonaromatic heterocycle-based energetic compounds,e.g.,hexahydro-1,3,5-trinitro-1,3,5-triazine(RDX)and octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine(HMX),whereas ethylene bridge is the core moiety of state-of-the-art explosive 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane(CL-20).In this context,it is of great interest to employ simple and practical bridges to assemble aromatic and nonaromatic nitrogen-rich heterocycles,thereby expanding the structural diversity of energetic materials,e.g.,bridged and fused nitrogen-rich poly-heterocycles.Furthermore,alkyl-bridged poly-heterocycles highlight the potential for the open chain type of energetic materials.In this review,the development of alkyl bridges in linking nitrogen-rich heterocycles is presented,and the perspective of the newly constructed energetic backbones is summarized for the future design of advanced energetic materials.展开更多
Azole fungicides(AFs)play an important role in the prevention and treatment of fungal diseases in agricultural crops.However,limited studies are addressing the fate and ecological risk of AFs in the urban water cycle ...Azole fungicides(AFs)play an important role in the prevention and treatment of fungal diseases in agricultural crops.However,limited studies are addressing the fate and ecological risk of AFs in the urban water cycle at a large watershed scale.To address this gap,we investigated the spatiotemporal distribution and ecological risk of twenty AFs in the lower reaches of the Yangtze River across four seasons.Carbendazim(CBA),tebuconazole(TBA),tricyclazole(TCA),and propiconazole(PPA)were found to be the dominant compounds.Their highest concentrations were measured in January(188.3 ng/L),and November(2197.1 ng/L),July(162.0 ng/L),and November(1801.9 ng/L),respectively.The comparison between wastewater treatment plants(WWTPs)effluents and surface water suggested that industrial WWTPs are major sources of AFs in the Yangtze River.In particular,TBA and PPA were found to be the most recalcitrant AFs in industrial WWTPs,while difenoconazole(DFA)was found to be the most potent pollutant in municipal WWTPs,with an average removal rate of less than60%.The average risk quotient(RQ)for the entire AFs was 6.45 in the fall,which was higher than in January(0.98),April(0.61),and July(0.40).This indicates that AFs in surface water posed higher environmental risks during the dry season.Additionally,the exposure risk of AFs via drinking water for sensitive populations deserves more attention.This study provides benchmark data on the occurrence of AFs in the lower reaches of the Yangtze River,and offers suggestions for better reduction of AFs.展开更多
Nitrogen-rich heterocyclic energetic compounds(NRHECs)and their salts have witnessed widespread synthesis in recent years.The substantial energy-density content within these compounds can lead to potentially dangerous...Nitrogen-rich heterocyclic energetic compounds(NRHECs)and their salts have witnessed widespread synthesis in recent years.The substantial energy-density content within these compounds can lead to potentially dangerous explosive reactions when subjected to external stimuli such as electrical discharge.Therefore,developing a reliable model for predicting their electrostatic discharge sensitivity(ESD)becomes imperative.This study proposes a novel and straightforward model based on the presence of specific groups(-NH_(2) or-NH-,-N=N^(+)-O^(-)and-NNO_(2),-ONO_(2) or-NO_(2))under certain conditions to assess the ESD of NRHECs and their salts,employing interpretable structural parameters.Utilizing a comprehensive dataset comprising 54 ESD measurements of NRHECs and their salts,divided into 49/5 training/test sets,the model achieves promising results.The Root Mean Square Error(RMSE),Mean Absolute Error(MAE),and Maximum Error for the training set are reported as 0.16 J,0.12 J,and 0.5 J,respectively.Notably,the ratios RMSE(training)/RMSE(test),MAE(training)/MAE(test),and Max Error(training)/Max Error(test)are all greater than 1.0,indicating the robust predictive capabilities of the model.The presented model demonstrates its efficacy in providing a reliable assessment of ESD for the targeted NRHECs and their salts,without the need for intricate computer codes or expert involvement.展开更多
Azole derivatives such as 2-mercaptobenzothiazole(MBT) and 2-mercaptobenzimidazole(MBI) were introduced as corrosion inhibitors into the interlayer space of sodium montmorillonite clay(Na+-MMT). The corrosion protecti...Azole derivatives such as 2-mercaptobenzothiazole(MBT) and 2-mercaptobenzimidazole(MBI) were introduced as corrosion inhibitors into the interlayer space of sodium montmorillonite clay(Na+-MMT). The corrosion protection behavior of mild steel in solutions containing MBT, MBI, MMT + MBT, MMT + MBI, Na^+-MMT, and NaCl(3.5 wt%) was evaluated using polarization and electrochemical impedance spectroscopy(EIS). Also, the release of penetrated species into the medium from the clay nanocarriers was evaluated using ultraviolet-visible(UV-Vis) spectroscopy. Small-angle X-ray scattering(SAXS) confirmed the insertion of MBT and MBI into the inner space of the clay layers and the interaction between two organic and inorganic phases. Scanning electron microscopy(SEM) was used to assess the morphology of the surface of the steel samples after the samples had been immersed for 24 h in the extraction solution. The corrosion protection in the solutions with clay nanocarriers containing MBT and MBI was better than that in solutions without MMT. The UV-Vis results showed that the release of MBI species from Na+-MMT nanocarriers in neutral pH was far lower than that of MBT species.展开更多
Rechargeable lithium-sulfur(Li-S)batteries are considered one of the most promising energy storage techniques owing to the high theoretical energy density.However,challenges still remain such as the shuttle effect of ...Rechargeable lithium-sulfur(Li-S)batteries are considered one of the most promising energy storage techniques owing to the high theoretical energy density.However,challenges still remain such as the shuttle effect of lithium polysulfides(LPSs)and the instability of lithium metal anode.Herein,we propose to use nitrogen-rich azoles,i.e.,triazole(Ta)and tetrazole(Tta),as trifunctional electrolyte additives for Li-S batteries.The azoles afford strong lithiophilicity for the chemisorption of LPSs.The density functional theory and experimental analysis verify the presence of Li bonds between the azoles and LPSs.The azoles can also interact with lithium salt in the electrolyte,leading to increase ionic conductivity and lithiumion transference number.Moreover,the azoles render particle-like lithium deposition on the lithium metal anode,leading to superlong cycling of a Li symmetric cell.The Li-S batteries with Ta and Tta exhibit the initial discharge capacity of 1425.5 and 1322.2 m Ah g^(-1),respectively,at 0.2 C rate,and promising cycling stability.They also enable enhanced cycling performance of a Li-organosulfide battery.展开更多
Antifungal drug resistance is a significant clinical problem, and antifungal agents that can evade resistance are urgently needed. In infective niches, resistant organisms often co-existed with sensitive ones, or a su...Antifungal drug resistance is a significant clinical problem, and antifungal agents that can evade resistance are urgently needed. In infective niches, resistant organisms often co-existed with sensitive ones, or a subpopulation of antibiotic-susceptible organisms may evolve into resistant ones during antibiotic treatment and eventually dominate the whole population. In this study, we established a co-culture assay in which an azole-resistant Candida albicans strain was mixed with a susceptible strain labeled with green fluorescent protein to mimic in vivo conditions and screen for antifungal drugs. Fluconazole was used as a positive control to verify the validity of this co-culture assay. Five natural molecules exhibited antifungal activity against both susceptible and resistant C. albicans. Two of these compounds, retigeric acid B(RAB) and riccardin D(RD), preferentially inhibited C. albicans strains in which the efflux pump MDR1 was activated. This selectivity was attributed to greater intracellular accumulation of the drugs in the resistant strains. Changes in sterol and lipid compositions were observed in the resistant strains compared to the susceptible strain, and might increase cell permeability to RAB and RD. In addition, RAB and RD interfered with the sterol pathway, further aggregating the decrease in ergosterol in the sterol synthesis pathway in the MDR1-activated strains. Our findings here provide an alternative for combating resistant pathogenic fungi.展开更多
Widespread use of azole fungicides and low removal efficiency in wastewater treatment plants(WWTPs) have led to the elevated concentration of azole fungicides in receiving environment. However, there was limited resea...Widespread use of azole fungicides and low removal efficiency in wastewater treatment plants(WWTPs) have led to the elevated concentration of azole fungicides in receiving environment. However, there was limited research about the removal mechanism of azole fungicides in the biological treatment of WWTPs. Imidazole fungicide climbazole and triazole fungicide fluconazole were selected to investigate the biodegradation mechanism of azole fungicides in activated sludge under aerobic conditions. Climbazole was found to be adsorbed to solid sludge and resulted in quick biodegradation. The degradation of climbazole in the aerobic activated sludge system was fitted well by the first-order kinetic model with a half-life of 5.3 days, while fluconazole tended to stay in liquid and had only about 30% of loss within 77 days incubation. Ten biotransformation products of climbazole were identified by high resolution mass spectrometry using suspect and non-target screening method. But no biodegradation products of fluconazole were identified due to its limited removal. The possible biodegradation pathways for climbazole were proposed based on the products identification and pathway prediction system, and involves oxidative dehalogenation, side chain oxidation and azole ring loss. The findings from this study suggest that it should be a concern for the persistence of fluconazole in the environment.展开更多
Ribavirin has been used in urgency to treat SARS patients recently.In order to study its antiviral mechanism by photolabeling approach,we have synthesized and characterized 5-azido-1-β-D-ribofuranosyl-1,2,4-triazole-...Ribavirin has been used in urgency to treat SARS patients recently.In order to study its antiviral mechanism by photolabeling approach,we have synthesized and characterized 5-azido-1-β-D-ribofuranosyl-1,2,4-triazole-3-carboxiamide 1 as a photolabeling probe of ribavirin.The azidotriazole nucleoside showed rapid and clean photochemical reaction,suggesting that l is a promising probe to study the antiviral mechanism of ribarivin by photolabeling.展开更多
Cardiac toxicity is an uncommon side effect of anti-fungal therapy. Until the recent reports of itraconazole (ITZ) associated cardiac failure, amphotericin was the antifungal most frequently reported with arrhythmias....Cardiac toxicity is an uncommon side effect of anti-fungal therapy. Until the recent reports of itraconazole (ITZ) associated cardiac failure, amphotericin was the antifungal most frequently reported with arrhythmias. We evaluated the cardiac effect of azole antifungals, specifically ITZ, and possible mechanisms of toxicity. Ex vivo live-heart studies were performed utilizing Sprague Dawley rats. Short exposure (<5 minutes), random crossover, dose ranging studies were performed with each pharmacologic agent. ITZ focused trials also included dose ranging utilizing a non-crossover design. The only azole found to have significant toxicity was ITZ. At ITZ ~ ED25 (2 - 2.5 ug/mL) exposures, contractility decreased by 22.2% ± 15.7% and amplitude of left ventricular pressure decreased by 11% ± 0.17%. Electron micrograph and alterations in mitochondrial respiration suggest mitochondrial toxicity as an underlying mechanism. In conclusion, ITZ was associated with reductions in contractility, possibly secondary to mitochondrial dysfunction and dilated cardiomyopathy.展开更多
Objective: To appraise the activity of voriconazole against Leishmania major(L. major) in vitro and its effectiveness on wound regeneration in cutaneous leishmaniasis in BALB/c mice Methods: The IC_(50) of voriconazol...Objective: To appraise the activity of voriconazole against Leishmania major(L. major) in vitro and its effectiveness on wound regeneration in cutaneous leishmaniasis in BALB/c mice Methods: The IC_(50) of voriconazole against promastigotes and intra-macrophage amastigotes of L. major was investigated in vitro. The in vivo study was performed by treating the L. major infected BALB/c mice. When the wounds appeared in the base of tail, treatment was started by administration of 30 mg/kg voriconazole for 28 consecutive days orally. Results: The IC_(50) of voriconazole against promastigotes and intra-macrophage amastigotes were 0.74 and 0.89μM, respectively. Voriconazole decreased lipid peroxidation and IL-6 level. Histopathologica findings indicated accelerated healing in the voriconazole treated group compared to other groups. Conclusions: Our results demonstrate that voriconazole can be an option in treating the cutaneous leishmaniasis by L. major.展开更多
Objective: To investigate the azole susceptibility of Candida albicans(C.albicans)from vulvovaginal candidosis patients and to analyze the relationship between ERG11 gene mutations in these isolates and azole resistan...Objective: To investigate the azole susceptibility of Candida albicans(C.albicans)from vulvovaginal candidosis patients and to analyze the relationship between ERG11 gene mutations in these isolates and azole resistance.Methods: Three hundred and two clinical isolates of Candida species were collected.Azole susceptibility was tested in vitro in microdilution studies. The ERG11 genes of 17 isolates of C. albicans(2 susceptibles, 5 dose-dependent resistants and 10 resistants) were amplified and sequenced.Results: Of the 302 isolates collected, 70.2% were C. albicans, of which 8.5%, 3.8% and4.2% were resistant to fluconazole, itraconazole and voriconazole, respectively. In total,27 missense mutations were detected in ERG11 genes from resistant/susceptible dosedependent isolates. Among them, Y132 H, A114 S, and Y257 H substitutions were most prevalent and were known to cause fluconazole resistance. G464 S and F72 S also have been proved to cause fluconazole resistance. Two novel substitutions(T285A, S457P) in hotspot regions were identified.Conclusions: Twenty seven mutations in the ERG11 gene were identified in azoleresistant C. albicans isolates, which indicated a possible relation with the increase in resistance to azole drugs and the recurrence of vulvovaginal candidosis. The relationship of two novel substitutions(T285A, S457P) with fluconazole resistance needs to be further verified by site-directed mutagenesis.展开更多
Triadimefon(TDM)and cyproconazole(CPZ)are two triazoles widely used as fungicides.Several azoles were synthe-sised starting from commercial TDM and CPZ.The compounds were evaluated against phytopathogenic filamentous ...Triadimefon(TDM)and cyproconazole(CPZ)are two triazoles widely used as fungicides.Several azoles were synthe-sised starting from commercial TDM and CPZ.The compounds were evaluated against phytopathogenic filamentous fungi,including Aspergillus fumigatus(AF),A.niger(AN),A.ustus(AU),A.japonicus(AJ),A.terreus(AT),Fusarium oxyspo-rum and Botrytis cinerea isolated from grapevine in the province of San Juan,Argentina.Three of the synthesised compounds(1-(Biphenyl-4-yloxy)-3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one,1;2-(Biphenyl-4-yl)-3-cyclopropyl-1-(1H-1,2,4-triazol-1-yl)butan-2-ol,3;3-Cyclopropyl-2-(4’-fluorobiphenyl-4-yl)-1-(1H-1,2,4-triazol1-yl)butan-2-ol,4)presented remarkable in vitro fungicidal properties,with better effects than TDM and CPZ on some of the target fungi.Cytotoxicity was assessed using human lung fibroblasts MRC5.Derivative 1,with IC50 values of 389.4μM,was less toxic towards MRC-5 human lung fibroblasts than commercial TDM(248.5μM)and CPZ(267.4μM).Docking analysis and molecular dynamics simulations suggest that the compounds present the same interaction in the binding pocket of the CYP51B enzyme and with the same amino acids as CPZ.The derivatives investigated could be considered broad-spectrum but with some selectivity towards imperfect fungi.展开更多
Background: The clinical significance of the detection of Candida albicans on mucous membranes of the respiratory or intestinal tract from patients in intensive care units is still not finally clarified. Many patients...Background: The clinical significance of the detection of Candida albicans on mucous membranes of the respiratory or intestinal tract from patients in intensive care units is still not finally clarified. Many patients reveal colonization, although, despite increased risk, there are only a few invasive infections detectable. Therefore, antimycotic therapy in this setting is strongly discouraged. In reality, however, many patients receive antimycotics as a pre-emptive therapy. To elucidate this point, a literature research was performed. Results: In the light of new results on the pathogenicity of C.albicans, the recommendation not to treat should be discussed anew. Without becoming invasive, C.albicans influences the immune system negatively in an anti-inflammatory sense (Th2) by means of at least two distinct mechanisms [action on toll like receptors (TLR), production of farnesol], which will be discussed. Conclusion: It is believed that patients in the phase of CARS or MARS can be further endangered by concomitant colonization of mucous membranes by C.albicans, i.e., in the sense of an anti-inflammatory immune response. Treatment with azole preparations, like fluconazole, which interacts with ergosterol synthesis in this phase of the disease, may trigger an additional effect on the patient, through increase of farnesol concentration by way of a negative feedback. Results of animal experiments on the immune system and concomitant therapeutic consequences indicate the need for verification through clinical trials.展开更多
Aim: Candida, an opportunistic organism is one of the commonest causes of hospital acquired infections among fungi. Currently available antifungal drugs have numerous adverse effects and drug-drug interactions (DDIs) ...Aim: Candida, an opportunistic organism is one of the commonest causes of hospital acquired infections among fungi. Currently available antifungal drugs have numerous adverse effects and drug-drug interactions (DDIs) along with increase in resistance over the time. Therefore, it is highly emergent to consider alternative treatments for candidal infections, having fewer adverse effects and is cost-effective. The current in-vitro study is undertaken to assess and compare the antifungal effects of the herbs, Berberis aristata (B. aristata, Darehald/Darhald) and Punica granatum (P. granatum, Pomegranate) with fluconazole and voriconazole, based on culture and sensitivity of candidal isolates. Materials and Methods: Ethanolic extracts of herbs (Berberis aristata and Punica granatum) and concentrations were formulated as per standard procedure. 130 samples were obtained for the study from in and out patients reported in clinical subsets of Ziauddin Hospital, Karachi from March to May, 2018. Samples were collected and grown according to the standard procedures like, wet mount test and gram’s staining. Species were identified by CHROM agar candida and API 20 C AUX methods. Sensitivity tests were performed by Kirby Bauer’s disc diffusion method according to CLSI guide lines M-44 A2, 2009. Data analysis was done by one-way ANOVA to compare the antifungal activities of drugs and herbs. Results: Mean inhibitory zones of herbs, B. aristata and P. granatum were highly significant against clinical candidal isolates with respective p-values of 0.00 and 0.02. Both of the herbs, B. aristata and P. granatum were found to be more sensitive, 98.5% and 97.7% respectively in comparison to fluconazole showing 42.3% and voriconazole showing 29.2% sensitivity against candidal isolates. The most resistant candidal specie was C. tropicalis that showed resistance against both fluconazole and voriconazole, contrary to that, this specie was highly sensitive to both of the herbs, showing sensitivity of 100% respective for Darehald and Pomegranate. Conclusion: In comparison to azoles: Culture sensitivity of both herbs (B. aristata and P. granatum) displayed more sensitivity against candidal isolates of patients having non-invasive and invasive candidiasis. These herbs can be considered as substitute or alternative antifungal agents to the conventional antifungal therapy, particularly in cases of treating candidemia patients, which is a life threating condition.展开更多
Some azoles were tested such as 3-amino-1,2,4-triazole (ATA), 3-4’-bitriazole -1,2,4 (BiTA)and 2-Mercaptobenzimidazole (MBI) against Cu-30Ni alloy corrosion in 3%NaCl polluted by ammonia using potentiodynamic measure...Some azoles were tested such as 3-amino-1,2,4-triazole (ATA), 3-4’-bitriazole -1,2,4 (BiTA)and 2-Mercaptobenzimidazole (MBI) against Cu-30Ni alloy corrosion in 3%NaCl polluted by ammonia using potentiodynamic measurements and electrochemical impedance spectroscopy and non-electrochemical techniques (scanning Electron Microscopy (SEM)) studied surface morphology has been used to characterize electrode surface. This study permitted to follow the evolution of the inhibitory effect of some azoles, on Cu-30Ni alloy corrosion in 3%NaCl polluted by ammonia and indicate that the tested inhibitors act as a good mixed-type inhibitor retarding the anodic and cathodic reactions. An increase of the inhibitors concentration leads to a decrease of corrosion rate and inhibition efficiency increase.展开更多
基金support of this work by the National Natural Science Foundation of China(Nos.22371307,21971267)the program for Guangdong Introducing Innovative and Entrepreneurial Teams(No.2017ZT07C069).
文摘Selective defluorinative functionalization of trifluoromethylarenes(ArCF3)to obtain the pharmaceutically commonα,α-difluorobenzylic motif is an attractive and elegant synthetic route.Over the past decade,although C(sp^(3))-F bonds functionalization have been greatly developed,catalytic cross-coupling of trifluoromethylarenes with C-H of terminal alkynes remains a challenge.Here,we report an approach to achieve Sonogashira-type cross-coupling of trifluoromethylarenes with terminal alkynes C(sp)-H bonds via photoredox and Cu/L dual catalysis.Tridentate anionic ligand is pivotal to realize this C-H sp-sp^(3) cross-coupling.Moreover,this unique catalytic system is also suitable for cross-coupling of C(sp^(3))-F bonds with azoles C(sp^(2))-H bonds.A series of trifluoromethylarenes,terminal alkynes and azoles with various functional groups are compatible with this protocol affording a variety of defluoroalkynylation or defluoroazolation products.Preliminary mechanistic studies indicated that deprotonated BINOL involved as a photocatalyst to activate ArCF3 rather than a ligand to the metal.
基金This work was supported by the National Natural Science Foundation of China(21901052,81872759)the Guangdong Province Universities and Colleges Pearl River Scholar Funded Scheme(2019)+1 种基金the Guangzhou Education Bureau University Scientific Research Project(201831845)the Guangdong Basic and Applied Basic Research Foundation(2020A1515010722).
文摘The installation of azoles via C–H/N–H cross-coupling is significantly underdeveloped,particularly in benzylic C–H azolation due to the requirement for external chemical oxidants and the challenge in controlling the site-and chemo-selectivity.Herein,a late-stage azolation of benzylic C‒H bonds enabled by electrooxidation is described,which proceeds in an undivided cell under mild,catalyst-and chemical-oxidant-free reaction conditions.The strategy empowers the C‒H azolation on primary,secondary,and even challenging tertiary benzylic positions selectively.The remarkable synthetic utility of our approach is highlighted by its easy scalability without overoxidation of products and ample scope with valuable functional groups.The approach can be directly used to install benzyl and azole motifs on highly functionalized drug molecules.
文摘Background: Vulvovaginal candidiasis (VVC) is a common cause of significant morbidity, affecting millions of women worldwide. It is estimated that approximately 75%of women of childbearing age will have at least one episode of candidiasis in their lifetime. In the last decades, resistance to azoles has become a public health problem. Although studies on vulvovaginitis have been done, there is lack of VVC studies in our area. The aim of this study was to describe the etiological and resistance profiles of vulvovaginal candidiasis to standard antifungus at the Saint Camille Hospital of Ouagadougou (HOSCO), Burkina Faso. Methods: We conducted a prospective study from January 2018 to December 2022. From vulvovaginal swabs, Candida species were identified using the ChromID® Candida Agar medium and the API® Candida gallery. Antifungal susceptibility testing was performed using Kirby-Bauer agar disk diffusion. Results: A total of 4789 women were sampled. The average age of sexually active women was 27.80+/−6.77 years, with extremes ranging from 15 to 64 years. Vaginal Candida infections accounted for 74.16% of the cases. The 20 - 29 age group was the most affected by vulvovaginal candidiasis. Pregnant women accounted for 28.76% of our study population. Women in the second (2nd) trimester of pregnancy had more Candida infections. Candida albicans was the most isolated species (55.12%), followed by Candida glabrata (27.64%), Candida tropicalis (6.91%), Candida famata (6.67%), Candida krusei (2.56%). All the Candida species isolated showed very high of resistance to Fluconazole (45.2%), Miconazole (23.7%) and Clotrimazole (45.7%). Conclusion: Species-specific antifungal results should always be considered to avoid antifungal resistance associated with vulvovaginal candidiasis. Identifying the causative species using vaginal fungal cultures can help guide therapy and improve outcomes for these patients.
基金support of the National Natural Science Foundation of China(Nos.22378369 and 22205207)Major Project of Natural Science Foundation of Zhejiang Province(LD24B060001).
文摘As an important chemical product,propylene(C_(3)H_(6))is widely used in production of many crucial chemical products such as polypropylene.Propane(C_(3)H_(8))is introduced as an inevitable gas impurity during the naphtha cracking in propylene production.At present,thermal-driven energy-intensive cryogenic distillation is the most common purification method in industry.An energy-efficient,cost-effective and environmental-friendly separation technology is required to get polymer grade C_(3)H_(6)(higher than 99.5%).In face of the increasing demand of propylene,new separation technology based on porous adsorbents is expected to be a promising alternative.In recent years,metal-organic frameworks(MOFs)have obtained attention by their high porosity,regular adjustable pore shape and pore environment and keep making breakthroughs in separation and purification of many industrial gas mixtures,and are thus considered as one of the most potential types of adsorbents.The physical properties of C_(3)H_(6)and C_(3)H_(8),such as boiling point,size and kinetic diameter,are close to each other,making their separation a challenge.Most C_(3)H_(6)/C_(3)H_(8)sieving MOFs based on narrow sieving channels that restrict the access of molecules larger than their confined entrance purify mixtures at the cost of diffusion and capacity.To improve the adsorption of MOFs based on molecular sieving,a novel‘pearl-necklace’strategy was designed,which was named for its connected channel and molecular pocket vividly,but the diffusion limitation remains unsolved.
基金National Natural Science Foundation of China(Grant Nos.22075023,22205022,and 22235003)to provide fund for conducting experiments。
文摘From the standpoint of chemical structures,the organic backbones of energetic materials can be classified into aromatic rings,nonaromatic rings,and open chains.Although the category of aromatic energetic compounds exhibits several advantages in the regulation of energetic properties,the nonaromatic heterocycles,assembling nitramino explosophores with simple alkyl bridges,still have prevailed in benchmark materials.The methylene bridge plays a pivotal role in the constructions of the classic nonaromatic heterocycle-based energetic compounds,e.g.,hexahydro-1,3,5-trinitro-1,3,5-triazine(RDX)and octahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine(HMX),whereas ethylene bridge is the core moiety of state-of-the-art explosive 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane(CL-20).In this context,it is of great interest to employ simple and practical bridges to assemble aromatic and nonaromatic nitrogen-rich heterocycles,thereby expanding the structural diversity of energetic materials,e.g.,bridged and fused nitrogen-rich poly-heterocycles.Furthermore,alkyl-bridged poly-heterocycles highlight the potential for the open chain type of energetic materials.In this review,the development of alkyl bridges in linking nitrogen-rich heterocycles is presented,and the perspective of the newly constructed energetic backbones is summarized for the future design of advanced energetic materials.
基金supported by the National Natural Science Foundation of China(Nos.52270072,4222780043)。
文摘Azole fungicides(AFs)play an important role in the prevention and treatment of fungal diseases in agricultural crops.However,limited studies are addressing the fate and ecological risk of AFs in the urban water cycle at a large watershed scale.To address this gap,we investigated the spatiotemporal distribution and ecological risk of twenty AFs in the lower reaches of the Yangtze River across four seasons.Carbendazim(CBA),tebuconazole(TBA),tricyclazole(TCA),and propiconazole(PPA)were found to be the dominant compounds.Their highest concentrations were measured in January(188.3 ng/L),and November(2197.1 ng/L),July(162.0 ng/L),and November(1801.9 ng/L),respectively.The comparison between wastewater treatment plants(WWTPs)effluents and surface water suggested that industrial WWTPs are major sources of AFs in the Yangtze River.In particular,TBA and PPA were found to be the most recalcitrant AFs in industrial WWTPs,while difenoconazole(DFA)was found to be the most potent pollutant in municipal WWTPs,with an average removal rate of less than60%.The average risk quotient(RQ)for the entire AFs was 6.45 in the fall,which was higher than in January(0.98),April(0.61),and July(0.40).This indicates that AFs in surface water posed higher environmental risks during the dry season.Additionally,the exposure risk of AFs via drinking water for sensitive populations deserves more attention.This study provides benchmark data on the occurrence of AFs in the lower reaches of the Yangtze River,and offers suggestions for better reduction of AFs.
文摘Nitrogen-rich heterocyclic energetic compounds(NRHECs)and their salts have witnessed widespread synthesis in recent years.The substantial energy-density content within these compounds can lead to potentially dangerous explosive reactions when subjected to external stimuli such as electrical discharge.Therefore,developing a reliable model for predicting their electrostatic discharge sensitivity(ESD)becomes imperative.This study proposes a novel and straightforward model based on the presence of specific groups(-NH_(2) or-NH-,-N=N^(+)-O^(-)and-NNO_(2),-ONO_(2) or-NO_(2))under certain conditions to assess the ESD of NRHECs and their salts,employing interpretable structural parameters.Utilizing a comprehensive dataset comprising 54 ESD measurements of NRHECs and their salts,divided into 49/5 training/test sets,the model achieves promising results.The Root Mean Square Error(RMSE),Mean Absolute Error(MAE),and Maximum Error for the training set are reported as 0.16 J,0.12 J,and 0.5 J,respectively.Notably,the ratios RMSE(training)/RMSE(test),MAE(training)/MAE(test),and Max Error(training)/Max Error(test)are all greater than 1.0,indicating the robust predictive capabilities of the model.The presented model demonstrates its efficacy in providing a reliable assessment of ESD for the targeted NRHECs and their salts,without the need for intricate computer codes or expert involvement.
文摘Azole derivatives such as 2-mercaptobenzothiazole(MBT) and 2-mercaptobenzimidazole(MBI) were introduced as corrosion inhibitors into the interlayer space of sodium montmorillonite clay(Na+-MMT). The corrosion protection behavior of mild steel in solutions containing MBT, MBI, MMT + MBT, MMT + MBI, Na^+-MMT, and NaCl(3.5 wt%) was evaluated using polarization and electrochemical impedance spectroscopy(EIS). Also, the release of penetrated species into the medium from the clay nanocarriers was evaluated using ultraviolet-visible(UV-Vis) spectroscopy. Small-angle X-ray scattering(SAXS) confirmed the insertion of MBT and MBI into the inner space of the clay layers and the interaction between two organic and inorganic phases. Scanning electron microscopy(SEM) was used to assess the morphology of the surface of the steel samples after the samples had been immersed for 24 h in the extraction solution. The corrosion protection in the solutions with clay nanocarriers containing MBT and MBI was better than that in solutions without MMT. The UV-Vis results showed that the release of MBI species from Na+-MMT nanocarriers in neutral pH was far lower than that of MBT species.
基金supported by the National Natural Science Foundation of China(Grant Nos.U2004214,21975225,and 51902293)。
文摘Rechargeable lithium-sulfur(Li-S)batteries are considered one of the most promising energy storage techniques owing to the high theoretical energy density.However,challenges still remain such as the shuttle effect of lithium polysulfides(LPSs)and the instability of lithium metal anode.Herein,we propose to use nitrogen-rich azoles,i.e.,triazole(Ta)and tetrazole(Tta),as trifunctional electrolyte additives for Li-S batteries.The azoles afford strong lithiophilicity for the chemisorption of LPSs.The density functional theory and experimental analysis verify the presence of Li bonds between the azoles and LPSs.The azoles can also interact with lithium salt in the electrolyte,leading to increase ionic conductivity and lithiumion transference number.Moreover,the azoles render particle-like lithium deposition on the lithium metal anode,leading to superlong cycling of a Li symmetric cell.The Li-S batteries with Ta and Tta exhibit the initial discharge capacity of 1425.5 and 1322.2 m Ah g^(-1),respectively,at 0.2 C rate,and promising cycling stability.They also enable enhanced cycling performance of a Li-organosulfide battery.
基金funded by the National Natural Science Foundation(Nos.81630093,81773786,81402804)the Young Scholars Program of Shandong University
文摘Antifungal drug resistance is a significant clinical problem, and antifungal agents that can evade resistance are urgently needed. In infective niches, resistant organisms often co-existed with sensitive ones, or a subpopulation of antibiotic-susceptible organisms may evolve into resistant ones during antibiotic treatment and eventually dominate the whole population. In this study, we established a co-culture assay in which an azole-resistant Candida albicans strain was mixed with a susceptible strain labeled with green fluorescent protein to mimic in vivo conditions and screen for antifungal drugs. Fluconazole was used as a positive control to verify the validity of this co-culture assay. Five natural molecules exhibited antifungal activity against both susceptible and resistant C. albicans. Two of these compounds, retigeric acid B(RAB) and riccardin D(RD), preferentially inhibited C. albicans strains in which the efflux pump MDR1 was activated. This selectivity was attributed to greater intracellular accumulation of the drugs in the resistant strains. Changes in sterol and lipid compositions were observed in the resistant strains compared to the susceptible strain, and might increase cell permeability to RAB and RD. In addition, RAB and RD interfered with the sterol pathway, further aggregating the decrease in ergosterol in the sterol synthesis pathway in the MDR1-activated strains. Our findings here provide an alternative for combating resistant pathogenic fungi.
基金supported by the National Natural Science Foundation of China(Nos.41473105,41877358 and 21806043)Scientific Research and Technology Development Program of Guangxi(No.2018AB36018)+1 种基金Guangdong Provincial Key Laboratory of Chemical Pollution and Environmental Safety(No.2019B030301008)the Pearl River Talent Plan of Guangdong Province(No.2017GC010244)。
文摘Widespread use of azole fungicides and low removal efficiency in wastewater treatment plants(WWTPs) have led to the elevated concentration of azole fungicides in receiving environment. However, there was limited research about the removal mechanism of azole fungicides in the biological treatment of WWTPs. Imidazole fungicide climbazole and triazole fungicide fluconazole were selected to investigate the biodegradation mechanism of azole fungicides in activated sludge under aerobic conditions. Climbazole was found to be adsorbed to solid sludge and resulted in quick biodegradation. The degradation of climbazole in the aerobic activated sludge system was fitted well by the first-order kinetic model with a half-life of 5.3 days, while fluconazole tended to stay in liquid and had only about 30% of loss within 77 days incubation. Ten biotransformation products of climbazole were identified by high resolution mass spectrometry using suspect and non-target screening method. But no biodegradation products of fluconazole were identified due to its limited removal. The possible biodegradation pathways for climbazole were proposed based on the products identification and pathway prediction system, and involves oxidative dehalogenation, side chain oxidation and azole ring loss. The findings from this study suggest that it should be a concern for the persistence of fluconazole in the environment.
基金Financial support from Wuhan University,Cheung Kong Scholar Foundation and the CNRS is gratefully acknowledged
文摘Ribavirin has been used in urgency to treat SARS patients recently.In order to study its antiviral mechanism by photolabeling approach,we have synthesized and characterized 5-azido-1-β-D-ribofuranosyl-1,2,4-triazole-3-carboxiamide 1 as a photolabeling probe of ribavirin.The azidotriazole nucleoside showed rapid and clean photochemical reaction,suggesting that l is a promising probe to study the antiviral mechanism of ribarivin by photolabeling.
文摘Cardiac toxicity is an uncommon side effect of anti-fungal therapy. Until the recent reports of itraconazole (ITZ) associated cardiac failure, amphotericin was the antifungal most frequently reported with arrhythmias. We evaluated the cardiac effect of azole antifungals, specifically ITZ, and possible mechanisms of toxicity. Ex vivo live-heart studies were performed utilizing Sprague Dawley rats. Short exposure (<5 minutes), random crossover, dose ranging studies were performed with each pharmacologic agent. ITZ focused trials also included dose ranging utilizing a non-crossover design. The only azole found to have significant toxicity was ITZ. At ITZ ~ ED25 (2 - 2.5 ug/mL) exposures, contractility decreased by 22.2% ± 15.7% and amplitude of left ventricular pressure decreased by 11% ± 0.17%. Electron micrograph and alterations in mitochondrial respiration suggest mitochondrial toxicity as an underlying mechanism. In conclusion, ITZ was associated with reductions in contractility, possibly secondary to mitochondrial dysfunction and dilated cardiomyopathy.
文摘Objective: To appraise the activity of voriconazole against Leishmania major(L. major) in vitro and its effectiveness on wound regeneration in cutaneous leishmaniasis in BALB/c mice Methods: The IC_(50) of voriconazole against promastigotes and intra-macrophage amastigotes of L. major was investigated in vitro. The in vivo study was performed by treating the L. major infected BALB/c mice. When the wounds appeared in the base of tail, treatment was started by administration of 30 mg/kg voriconazole for 28 consecutive days orally. Results: The IC_(50) of voriconazole against promastigotes and intra-macrophage amastigotes were 0.74 and 0.89μM, respectively. Voriconazole decreased lipid peroxidation and IL-6 level. Histopathologica findings indicated accelerated healing in the voriconazole treated group compared to other groups. Conclusions: Our results demonstrate that voriconazole can be an option in treating the cutaneous leishmaniasis by L. major.
基金Supported by the National Natural Science Foundation of China(No.31072125 and 31272549)by a National Science and Technology Project (China) grant (2008ZX-10004-011)
文摘Objective: To investigate the azole susceptibility of Candida albicans(C.albicans)from vulvovaginal candidosis patients and to analyze the relationship between ERG11 gene mutations in these isolates and azole resistance.Methods: Three hundred and two clinical isolates of Candida species were collected.Azole susceptibility was tested in vitro in microdilution studies. The ERG11 genes of 17 isolates of C. albicans(2 susceptibles, 5 dose-dependent resistants and 10 resistants) were amplified and sequenced.Results: Of the 302 isolates collected, 70.2% were C. albicans, of which 8.5%, 3.8% and4.2% were resistant to fluconazole, itraconazole and voriconazole, respectively. In total,27 missense mutations were detected in ERG11 genes from resistant/susceptible dosedependent isolates. Among them, Y132 H, A114 S, and Y257 H substitutions were most prevalent and were known to cause fluconazole resistance. G464 S and F72 S also have been proved to cause fluconazole resistance. Two novel substitutions(T285A, S457P) in hotspot regions were identified.Conclusions: Twenty seven mutations in the ERG11 gene were identified in azoleresistant C. albicans isolates, which indicated a possible relation with the increase in resistance to azole drugs and the recurrence of vulvovaginal candidosis. The relationship of two novel substitutions(T285A, S457P) with fluconazole resistance needs to be further verified by site-directed mutagenesis.
文摘Triadimefon(TDM)and cyproconazole(CPZ)are two triazoles widely used as fungicides.Several azoles were synthe-sised starting from commercial TDM and CPZ.The compounds were evaluated against phytopathogenic filamentous fungi,including Aspergillus fumigatus(AF),A.niger(AN),A.ustus(AU),A.japonicus(AJ),A.terreus(AT),Fusarium oxyspo-rum and Botrytis cinerea isolated from grapevine in the province of San Juan,Argentina.Three of the synthesised compounds(1-(Biphenyl-4-yloxy)-3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one,1;2-(Biphenyl-4-yl)-3-cyclopropyl-1-(1H-1,2,4-triazol-1-yl)butan-2-ol,3;3-Cyclopropyl-2-(4’-fluorobiphenyl-4-yl)-1-(1H-1,2,4-triazol1-yl)butan-2-ol,4)presented remarkable in vitro fungicidal properties,with better effects than TDM and CPZ on some of the target fungi.Cytotoxicity was assessed using human lung fibroblasts MRC5.Derivative 1,with IC50 values of 389.4μM,was less toxic towards MRC-5 human lung fibroblasts than commercial TDM(248.5μM)and CPZ(267.4μM).Docking analysis and molecular dynamics simulations suggest that the compounds present the same interaction in the binding pocket of the CYP51B enzyme and with the same amino acids as CPZ.The derivatives investigated could be considered broad-spectrum but with some selectivity towards imperfect fungi.
文摘Background: The clinical significance of the detection of Candida albicans on mucous membranes of the respiratory or intestinal tract from patients in intensive care units is still not finally clarified. Many patients reveal colonization, although, despite increased risk, there are only a few invasive infections detectable. Therefore, antimycotic therapy in this setting is strongly discouraged. In reality, however, many patients receive antimycotics as a pre-emptive therapy. To elucidate this point, a literature research was performed. Results: In the light of new results on the pathogenicity of C.albicans, the recommendation not to treat should be discussed anew. Without becoming invasive, C.albicans influences the immune system negatively in an anti-inflammatory sense (Th2) by means of at least two distinct mechanisms [action on toll like receptors (TLR), production of farnesol], which will be discussed. Conclusion: It is believed that patients in the phase of CARS or MARS can be further endangered by concomitant colonization of mucous membranes by C.albicans, i.e., in the sense of an anti-inflammatory immune response. Treatment with azole preparations, like fluconazole, which interacts with ergosterol synthesis in this phase of the disease, may trigger an additional effect on the patient, through increase of farnesol concentration by way of a negative feedback. Results of animal experiments on the immune system and concomitant therapeutic consequences indicate the need for verification through clinical trials.
文摘Aim: Candida, an opportunistic organism is one of the commonest causes of hospital acquired infections among fungi. Currently available antifungal drugs have numerous adverse effects and drug-drug interactions (DDIs) along with increase in resistance over the time. Therefore, it is highly emergent to consider alternative treatments for candidal infections, having fewer adverse effects and is cost-effective. The current in-vitro study is undertaken to assess and compare the antifungal effects of the herbs, Berberis aristata (B. aristata, Darehald/Darhald) and Punica granatum (P. granatum, Pomegranate) with fluconazole and voriconazole, based on culture and sensitivity of candidal isolates. Materials and Methods: Ethanolic extracts of herbs (Berberis aristata and Punica granatum) and concentrations were formulated as per standard procedure. 130 samples were obtained for the study from in and out patients reported in clinical subsets of Ziauddin Hospital, Karachi from March to May, 2018. Samples were collected and grown according to the standard procedures like, wet mount test and gram’s staining. Species were identified by CHROM agar candida and API 20 C AUX methods. Sensitivity tests were performed by Kirby Bauer’s disc diffusion method according to CLSI guide lines M-44 A2, 2009. Data analysis was done by one-way ANOVA to compare the antifungal activities of drugs and herbs. Results: Mean inhibitory zones of herbs, B. aristata and P. granatum were highly significant against clinical candidal isolates with respective p-values of 0.00 and 0.02. Both of the herbs, B. aristata and P. granatum were found to be more sensitive, 98.5% and 97.7% respectively in comparison to fluconazole showing 42.3% and voriconazole showing 29.2% sensitivity against candidal isolates. The most resistant candidal specie was C. tropicalis that showed resistance against both fluconazole and voriconazole, contrary to that, this specie was highly sensitive to both of the herbs, showing sensitivity of 100% respective for Darehald and Pomegranate. Conclusion: In comparison to azoles: Culture sensitivity of both herbs (B. aristata and P. granatum) displayed more sensitivity against candidal isolates of patients having non-invasive and invasive candidiasis. These herbs can be considered as substitute or alternative antifungal agents to the conventional antifungal therapy, particularly in cases of treating candidemia patients, which is a life threating condition.
文摘Some azoles were tested such as 3-amino-1,2,4-triazole (ATA), 3-4’-bitriazole -1,2,4 (BiTA)and 2-Mercaptobenzimidazole (MBI) against Cu-30Ni alloy corrosion in 3%NaCl polluted by ammonia using potentiodynamic measurements and electrochemical impedance spectroscopy and non-electrochemical techniques (scanning Electron Microscopy (SEM)) studied surface morphology has been used to characterize electrode surface. This study permitted to follow the evolution of the inhibitory effect of some azoles, on Cu-30Ni alloy corrosion in 3%NaCl polluted by ammonia and indicate that the tested inhibitors act as a good mixed-type inhibitor retarding the anodic and cathodic reactions. An increase of the inhibitors concentration leads to a decrease of corrosion rate and inhibition efficiency increase.