Thiazoles including five 2-arylbenzothiazoles and two 2-arylnaphthothiazoles were synthesized using a simple synthetic strategy in this work.2-Arylbenzothiazoles and 2-arylnaphthothiazoles can be prepared by the react...Thiazoles including five 2-arylbenzothiazoles and two 2-arylnaphthothiazoles were synthesized using a simple synthetic strategy in this work.2-Arylbenzothiazoles and 2-arylnaphthothiazoles can be prepared by the reaction of methylaromatics with aniline or naphthylamine in the presence of elemental sulfur,respectively.All the seven thiazoles were characterized by the melting point measurement,FTIR,~1H NMR,^（13）C NMR and GC-MS analysis.展开更多
A convenient solvent less cyclocondensation from thiosemicarbazone of benzofuranone and chloroacetic acid using an ionic liquid, N-methylpyridinium tosylate for obtaining novel 4-thiazolidinones in excellent yields is...A convenient solvent less cyclocondensation from thiosemicarbazone of benzofuranone and chloroacetic acid using an ionic liquid, N-methylpyridinium tosylate for obtaining novel 4-thiazolidinones in excellent yields is reported. Also, the green expedient synthesis of new 2,4-disubstituted thiazoles under grinding condition from phenacyl bromides and thiosemicarbazide derivatives in quantitative yields is reported.展开更多
Ketones smoothly reacted with NBS in the presence of a catalytic amount of ptoluenesulfonic acid to give α-bromoketones in good yields in typical ionic liquids, such as [bmim]PF6 and [bmpy]Tf2N, and the ionic liquids...Ketones smoothly reacted with NBS in the presence of a catalytic amount of ptoluenesulfonic acid to give α-bromoketones in good yields in typical ionic liquids, such as [bmim]PF6 and [bmpy]Tf2N, and the ionic liquids could be repeatedly used for the same reaction after the extraction of the α-bromoketones. Then, the one-pot conversion of ketones into thiazoles by the treatment with NBS, and subsequently with thioamides could be also carried out in [bmim]PF6 and [bmpy]Tf2N, respectively Thus, [bmim]PF6 and [bmpy]Tf2N could be used as recyclable reaction media for the preparation α-bromoketones and thiazoles from ketones.展开更多
Novel quinazolonthiazoles were designed and synthesized as new potential antimicrobial agents by facile multi-step procedure from o-aminobenzoic acids and 2-acetylthiazole.A series of biological evaluation showed that...Novel quinazolonthiazoles were designed and synthesized as new potential antimicrobial agents by facile multi-step procedure from o-aminobenzoic acids and 2-acetylthiazole.A series of biological evaluation showed that compound 7d was the most effective quinazolonethiazole with superior activity to reference drugs chloramphenicol and norfloxacin.This active molecule displayed unob-vious bacterial resistance against P.aeruginosa,the low toxicity to normal hepatocytes,suitable pharmacokinetics and drug-likeness.The preliminary biological interaction suggested that quinazolonethiazole 7d might induce bacterial death by disturbing the membrane permeability,whilst preventing bacteria from growth by integrating into DNA and binding with topoisomerase IV.These findings provided significant background for the further development of quinazolonethiazoles as new potential drugs in combating drug-resistant pathogens.展开更多
A high-efficient and stereo-specific approach for the preparation of biologically important （E）-2-styryl-tetra- hydrobenzo[d]thiazoles has been developed via TMSC1 promoted direct sp3 C-H alkenylation of 2-methyl-5,...A high-efficient and stereo-specific approach for the preparation of biologically important （E）-2-styryl-tetra- hydrobenzo[d]thiazoles has been developed via TMSC1 promoted direct sp3 C-H alkenylation of 2-methyl-5,6-di- hydrobenzo[d]thiazol-7（4H）-one under metal-free conditions. Seventeen target compounds were synthesized in ex- cellent yields of 82%--98% under the optimal conditions of 300 mol% TMSCI at 110℃ for 2 h, and their chemical structures were elucidated by IR, NMR, ESI-MS, elemental analyses and X-ray crystallography analysis. A plausible mechanism was also proposed, and this method provided a good functional group conversion for the sp3 C-H substrates.展开更多
Targeted construction of new covalent organic frameworks(COFs)with specific purposes and rationalities to build colorimetric assay platform for environmental pollutant monitoring have attracted increasing interest.How...Targeted construction of new covalent organic frameworks(COFs)with specific purposes and rationalities to build colorimetric assay platform for environmental pollutant monitoring have attracted increasing interest.However,it is still challenging due to lack of available coordination sites inside COFs pores and only a slight bonding ability for anchoring metal.In this work,a two-dimensional(2D)COFs(termed as Tz-COF)with high crystallinity,excellent chemical stability,and abundant sulfur coordination in its skeletons was synthesized and used for the confined growth of Au NPs.It was found that the Au NPs showed significant dispersibility for the support of Tz-COF.The proposed Tz-COF@Au NPs possessed outstanding Hg^(2+)-activated peroxidase-like activity benefited from physicochemical properties of gold amalgam and synergistic effect between COFs and Au NPs to oxidize chromogenic substrate.Based on highly efficient activity and distinctive color evolution,the strategy for detecting Hg^(2+)was developed and successfully applied to determine the content of Hg^(2+)in real environmental samples.This work manifests that a potential strategy to establish a colorimetric assay platform for environmental pollutant monitoring based on the targeted manufacturing of novel COFs with specific functions.展开更多
In order to screen out effective fungicides for controlling citrus canker,the control effects of 9 fungicides on Jinhong bingtang orange canker were studied.The results showed that 77%cupric calcium sulfate WP,30%copp...In order to screen out effective fungicides for controlling citrus canker,the control effects of 9 fungicides on Jinhong bingtang orange canker were studied.The results showed that 77%cupric calcium sulfate WP,30%copper oxychloride SC,46%copper hydroxide WG,30%thiodiazole-copper SC and 40%zinc thiazole SC had better comprehensive control effect on citrus canker,6%benziothiazolinone WG had an average effect,3%zhongshengmycin AS,2%kasugamycin AS and 33.5%oxine-copper SC had poor control effect.Therefore,fungicides could be used alternately or choose compounded preparation.In addition,adjuvants could be considered in use,which was an effective way to enhance efficacy,reduced dosage and delayed pesticide resistance.展开更多
Some new 2-thioxo thiazole, 2-thioxo 1,3,4- thiadiazole and 3-thioxo-1,3,4-triazole derivatives （3-17） have been synthesized through ring closure reactions ofdithioic formic acid hydrazones 2 with functional reagent...Some new 2-thioxo thiazole, 2-thioxo 1,3,4- thiadiazole and 3-thioxo-1,3,4-triazole derivatives （3-17） have been synthesized through ring closure reactions ofdithioic formic acid hydrazones 2 with functional reagents in different medium. Former structures of the products have been established by the help of elemental and spectral analysis. Most of the obtained targets showed a moderate activity towards some microbes in comparison with two antibiotics Pipercillin and Mycostatine.展开更多
DFT quantum chemical computations have been carried out at the B3LYP/6-31G (d) level. Full geometry optimization has been performed and equilibrium geometries for a new series of phenyl thiazoles have been located. Gr...DFT quantum chemical computations have been carried out at the B3LYP/6-31G (d) level. Full geometry optimization has been performed and equilibrium geometries for a new series of phenyl thiazoles have been located. Ground state electronic properties, charge density distributions, dipole moments and its components have been calculated and reported. Effect of substituents on the geometry and on the polarization of the studied series of compounds are analyzed and discussed. Some structural features have been pinpointed to underline the affinity and selectivity of the studied compounds as adenosine A3-receptor antagonists. Results of the present work indicate that activity towards A3 receptor sites is directly correlated with both of the polarity and the co-planarity of the thiazole.展开更多
Eleven new imine derivatives 6 containing 1H-1,2,4-triazole and thiazole rings were synthesized by the condensation of 5-((1H- 1,2,4-triazol-1-yl)methyl)-4-tert-butylthiazol-2-amine with various substituted benzaldehy...Eleven new imine derivatives 6 containing 1H-1,2,4-triazole and thiazole rings were synthesized by the condensation of 5-((1H- 1,2,4-triazol-1-yl)methyl)-4-tert-butylthiazol-2-amine with various substituted benzaldehydes.The structures of the title compounds were characterized by ~1H NMR,MS and elemental analysis.The plant-growth regulatory activities of these compounds were evaluated.The primary bioassay results indicated that these target compounds exhibited promising plant-growth regulatory activities.展开更多
A series of new pyrazole oximes bearing substituted thiazole ring were designed and prepared. The structures of the title compounds were identified by spectral analyses, The results of primary bioassay indicated that ...A series of new pyrazole oximes bearing substituted thiazole ring were designed and prepared. The structures of the title compounds were identified by spectral analyses, The results of primary bioassay indicated that some targeted compounds exhibited promising insecticidal activity besides acaricidal activity, particularly; compounds 8c and 8d were more potent against Tetranychus cinnabarinus and Plutella xylostella than other analogues.展开更多
The title compound 2-（1-（3-bromo-1-（3-chloropyridin-2-yl）-1H-pyrazole-5-carbonyl）piperidin-4-yl）-N-isopropylthiazole-4-carboxamide（C21H22Br Cl N6O2 S,Mr = 536.04） has been synthesized,and its structure was cha...The title compound 2-（1-（3-bromo-1-（3-chloropyridin-2-yl）-1H-pyrazole-5-carbonyl）piperidin-4-yl）-N-isopropylthiazole-4-carboxamide（C21H22Br Cl N6O2 S,Mr = 536.04） has been synthesized,and its structure was characterized by IR spectra,1H-NMR,13C-NMR,EA,and single-crystal X-ray diffraction.The crystal of the title compound belongs to monoclinic system,space group P/c with a = 15.146（3）,b = 11.573（2）,c = 26.937（5） A,β = 103.64（3）°,V = 1839.0（6） A^3,Z = 4,Dc = 1.557 g/cm^3,μ（Mo Ka） = 0.71073 mm^-1,F（000） = 2192,R = 0.0601 and w R = 0.1392.There exist one intramolecular hydrogen bond at N–H···N and four intermolecular weak interactions at O（2）···H（1）,Cl（1）···H（12）,O（1）···Cl（1） and S（1）···O（2）.Bioassay results indicated that the title compound had good fungicidal and antiviral activities against tobacco mosaic virus.展开更多
In recent decades, peptides as potential drugs were more and more explored with the development of non-oral medicine. There into, sulfur-containing peptide is one of the most popular aspects in peptide drugs due to th...In recent decades, peptides as potential drugs were more and more explored with the development of non-oral medicine. There into, sulfur-containing peptide is one of the most popular aspects in peptide drugs due to the introduction of sulfur atoms leading unique properties.The purpose of the present review is to focus on the discovery of various sulfur-containing peptides with particular emphasis on their pharmacological mechanisms. This review is organized according to the structures of the sulfurcontaining peptides.展开更多
The title compound 2, 4-chloromethyl-3-anilino-2-（4-methyl-benzoylimido）thiazole, was prepared by the reaction of 1-p-methylbenzoyl-3-phenylaminothiourea 1 with 1,3-dichloro- acetone. The crystal is of monoclinic, s...The title compound 2, 4-chloromethyl-3-anilino-2-（4-methyl-benzoylimido）thiazole, was prepared by the reaction of 1-p-methylbenzoyl-3-phenylaminothiourea 1 with 1,3-dichloro- acetone. The crystal is of monoclinic, space group P21/c, with a = 8.1712（15）, b = 10.998（2）, c = 19.134（4）A, β= 94.610（5）°, C18H16ClN3OS, Mr = 357.85, Z = 4, V = 1714.0（6）A^3, De= 1.387 g/cm^3, μ（MoKa） = 0.354 mm^-1, F（000） = 744, the final R = 0.0518 and wR = 0.1167 for 3189 observed reflections （I〉 2σ（I）. Its formation mechanism was proposed.展开更多
A new kind of aromatic diamine monomer containing thiazole unit, 2-amino-5-（4-aminophenyl）-thiazole （AAPT）, was synthesized in three steps, starting from 4-nitroacetophenone. A novel thiazole-containing polyimide ...A new kind of aromatic diamine monomer containing thiazole unit, 2-amino-5-（4-aminophenyl）-thiazole （AAPT）, was synthesized in three steps, starting from 4-nitroacetophenone. A novel thiazole-containing polyimide was prepared via the polycondensation of AAPT with 6FDA by one-step method. The resulting polyimide exhibits excellent solubility, film-forming capability and high thermal resistance.展开更多
A series of new biquinoline derivatives containing a thiazole moiety were synthesized by a one-pot,base-catalyzed cyclocondensation reaction of 2-chloro-3-formyl quinoline,malononitrile and enaminone.All the synthesiz...A series of new biquinoline derivatives containing a thiazole moiety were synthesized by a one-pot,base-catalyzed cyclocondensation reaction of 2-chloro-3-formyl quinoline,malononitrile and enaminone.All the synthesized compounds were characterized by elemental analysis,FT-IR,~1H NMR and ^（13）C NMR data.All the synthesized compounds were screened against three bacterial pathogens,namely Bacillus cereus,B.substilis and Escherichia coli and for antifungal activity against three fungal pathogens,Aspergillus niger,Fusarium oxisporum and Rhizopus using the disc diffusion method.展开更多
A derivative of thiazole（AAT） has been explored as a sensing material for preparation a selective Lu（III） PVC-based membrane sensor.The proposed sensor exhibits a Nernstian response over a wide concentration range...A derivative of thiazole（AAT） has been explored as a sensing material for preparation a selective Lu（III） PVC-based membrane sensor.The proposed sensor exhibits a Nernstian response over a wide concentration range from 1.0×10^（-6） to 1.0×10^（-1） mol/L of Lu（Ⅲ） and the detection limit is 5.7×10^（-7） mol/L.The sensor response is independent of pH of the solution in the range 3.2-8.8 and possesses the advantages of fast response time（～6） and in particular,good selectivity to the lutetium ions with regard to most common metal ions,and especially all lanthanide ions.展开更多
A new series of multi-heterocyclic Schiff base was constructed starting from 4＇-（imidazol-1-yl[56_TD$IF]）-acetophenone which was converted to its 2-bromoethanone precursor which on cyclic condensation with thiourea...A new series of multi-heterocyclic Schiff base was constructed starting from 4＇-（imidazol-1-yl[56_TD$IF]）-acetophenone which was converted to its 2-bromoethanone precursor which on cyclic condensation with thiourea yielded final thiazol-2-amine intermediate（3） to be reacted with substituted aldehydes to generate final imidazolylphenylheterocyclic-2-ylmethylenethiazole-2-amines（4a–4i）. New Schiff base was investigated for their in vitro cytotoxic efficacies against a panel of three human cancer cell lines namely, MCF7（human breast cancer）, HCT116（human colon cancer）, and DU145（human prostate cancer） and one normal skin fibroblast（SF）. Most of these synthetic derivatives shown important cytotoxic actions against individual carcinoma cell line collections, but weak actions against SF, which is as anticipated. Observations of SAR suggested that the difference in the characteristics of substituents attached to the Schiff base function leads to the interesting variations within pharmacological effects of resultant molecular systems. Structural analysis performed using FT-IR,~1H NMR,^（13）C NMR spectroscopy and CHN analysis for final potent anticancer Schiff base, which warrant further investigations.展开更多
The present work aimed to synthesize a new interesting series of thiazole based polyamides containing diarylidenecyclohexanone moiety 5a-5f using low temperature solution polycondensation technique. The new polymers w...The present work aimed to synthesize a new interesting series of thiazole based polyamides containing diarylidenecyclohexanone moiety 5a-5f using low temperature solution polycondensation technique. The new polymers were synthesized by the reaction of thiazole based monomer namely, bis（2-aminothiazol-4-ylbenzylidene）cyclohexanone 3 with different aliphatic and aromatic diacid chlorides using NMP, and in the presence of anhydrous Li Cl as catalyst. Adipoyl, sebacoyl, oxaloyl, terephthaloyl, isophthaloyl dichlorides and biphenyl dicarbonyl dichloride were used as diacid chlorides. The structure of the model compound 4 as well as the new polymers was confirmed by correct elemental and spectral analyses. The thermal properties of those polymers were evaluated by TGA and DTG measurements and correlated to their structural units, beside X-ray diffraction analysis, solubility and viscometry measurements. The inherent viscosities for the synthesized polymers were in the range 0.6–1.03 d L/g. On the other hand the corrosion inhibitive properties of monomer 3 as well as polyamides 5d and 5f as selected examples were carried out on carbon-steel in 0.5 mol/L H2SO4 at 40 °C. The calculated inhibition efficiency（IE%） for polymer 5d was in the range（82 ± 6）% in all selected concentrations. The best value of IE% was obtained at 1 mg/L to reach 98.24% for polymer 5d and at 0.5 mg/L to reach 87.75% for polymer 5f.展开更多
基金support from National Basic Research Program of China(973 Program, No2012CB214900)the National Natural Science Foundation of China(No21176246)the Fundamental Research Funds for the Central Universities
文摘Thiazoles including five 2-arylbenzothiazoles and two 2-arylnaphthothiazoles were synthesized using a simple synthetic strategy in this work.2-Arylbenzothiazoles and 2-arylnaphthothiazoles can be prepared by the reaction of methylaromatics with aniline or naphthylamine in the presence of elemental sulfur,respectively.All the seven thiazoles were characterized by the melting point measurement,FTIR,~1H NMR,^（13）C NMR and GC-MS analysis.
文摘A convenient solvent less cyclocondensation from thiosemicarbazone of benzofuranone and chloroacetic acid using an ionic liquid, N-methylpyridinium tosylate for obtaining novel 4-thiazolidinones in excellent yields is reported. Also, the green expedient synthesis of new 2,4-disubstituted thiazoles under grinding condition from phenacyl bromides and thiosemicarbazide derivatives in quantitative yields is reported.
文摘Ketones smoothly reacted with NBS in the presence of a catalytic amount of ptoluenesulfonic acid to give α-bromoketones in good yields in typical ionic liquids, such as [bmim]PF6 and [bmpy]Tf2N, and the ionic liquids could be repeatedly used for the same reaction after the extraction of the α-bromoketones. Then, the one-pot conversion of ketones into thiazoles by the treatment with NBS, and subsequently with thioamides could be also carried out in [bmim]PF6 and [bmpy]Tf2N, respectively Thus, [bmim]PF6 and [bmpy]Tf2N could be used as recyclable reaction media for the preparation α-bromoketones and thiazoles from ketones.
基金the National Natural Science Foundation of China(Nos.21971212 and 21672173)the Research Funds for the Central Universities(No.XDJK2020C031)+2 种基金the China Postdoctoral Science Foundation(No.2019M653821XB)the Postdoctoral Science Foundation Project of Chongqing Science and Technology Bureau(No.cstc2019jcyj-bshX0124)the Chongqing Special Foundation for Postdoctoral Research Proposal(No.XmT2018082).
文摘Novel quinazolonthiazoles were designed and synthesized as new potential antimicrobial agents by facile multi-step procedure from o-aminobenzoic acids and 2-acetylthiazole.A series of biological evaluation showed that compound 7d was the most effective quinazolonethiazole with superior activity to reference drugs chloramphenicol and norfloxacin.This active molecule displayed unob-vious bacterial resistance against P.aeruginosa,the low toxicity to normal hepatocytes,suitable pharmacokinetics and drug-likeness.The preliminary biological interaction suggested that quinazolonethiazole 7d might induce bacterial death by disturbing the membrane permeability,whilst preventing bacteria from growth by integrating into DNA and binding with topoisomerase IV.These findings provided significant background for the further development of quinazolonethiazoles as new potential drugs in combating drug-resistant pathogens.
基金The authors thank the finance supported by the National Natural Science Foundation of China （No. 21272136）, and Scientific Research Innovation Founda- tion of Graduate School of China Three Gorges Univer- sity.
文摘A high-efficient and stereo-specific approach for the preparation of biologically important （E）-2-styryl-tetra- hydrobenzo[d]thiazoles has been developed via TMSC1 promoted direct sp3 C-H alkenylation of 2-methyl-5,6-di- hydrobenzo[d]thiazol-7（4H）-one under metal-free conditions. Seventeen target compounds were synthesized in ex- cellent yields of 82%--98% under the optimal conditions of 300 mol% TMSCI at 110℃ for 2 h, and their chemical structures were elucidated by IR, NMR, ESI-MS, elemental analyses and X-ray crystallography analysis. A plausible mechanism was also proposed, and this method provided a good functional group conversion for the sp3 C-H substrates.
基金supported by the National Natural Science Foundation of China(Nos.22274021,21974021 and 22036001).
文摘Targeted construction of new covalent organic frameworks(COFs)with specific purposes and rationalities to build colorimetric assay platform for environmental pollutant monitoring have attracted increasing interest.However,it is still challenging due to lack of available coordination sites inside COFs pores and only a slight bonding ability for anchoring metal.In this work,a two-dimensional(2D)COFs(termed as Tz-COF)with high crystallinity,excellent chemical stability,and abundant sulfur coordination in its skeletons was synthesized and used for the confined growth of Au NPs.It was found that the Au NPs showed significant dispersibility for the support of Tz-COF.The proposed Tz-COF@Au NPs possessed outstanding Hg^(2+)-activated peroxidase-like activity benefited from physicochemical properties of gold amalgam and synergistic effect between COFs and Au NPs to oxidize chromogenic substrate.Based on highly efficient activity and distinctive color evolution,the strategy for detecting Hg^(2+)was developed and successfully applied to determine the content of Hg^(2+)in real environmental samples.This work manifests that a potential strategy to establish a colorimetric assay platform for environmental pollutant monitoring based on the targeted manufacturing of novel COFs with specific functions.
文摘In order to screen out effective fungicides for controlling citrus canker,the control effects of 9 fungicides on Jinhong bingtang orange canker were studied.The results showed that 77%cupric calcium sulfate WP,30%copper oxychloride SC,46%copper hydroxide WG,30%thiodiazole-copper SC and 40%zinc thiazole SC had better comprehensive control effect on citrus canker,6%benziothiazolinone WG had an average effect,3%zhongshengmycin AS,2%kasugamycin AS and 33.5%oxine-copper SC had poor control effect.Therefore,fungicides could be used alternately or choose compounded preparation.In addition,adjuvants could be considered in use,which was an effective way to enhance efficacy,reduced dosage and delayed pesticide resistance.
文摘Some new 2-thioxo thiazole, 2-thioxo 1,3,4- thiadiazole and 3-thioxo-1,3,4-triazole derivatives （3-17） have been synthesized through ring closure reactions ofdithioic formic acid hydrazones 2 with functional reagents in different medium. Former structures of the products have been established by the help of elemental and spectral analysis. Most of the obtained targets showed a moderate activity towards some microbes in comparison with two antibiotics Pipercillin and Mycostatine.
文摘DFT quantum chemical computations have been carried out at the B3LYP/6-31G (d) level. Full geometry optimization has been performed and equilibrium geometries for a new series of phenyl thiazoles have been located. Ground state electronic properties, charge density distributions, dipole moments and its components have been calculated and reported. Effect of substituents on the geometry and on the polarization of the studied series of compounds are analyzed and discussed. Some structural features have been pinpointed to underline the affinity and selectivity of the studied compounds as adenosine A3-receptor antagonists. Results of the present work indicate that activity towards A3 receptor sites is directly correlated with both of the polarity and the co-planarity of the thiazole.
基金the National Natural Science Foundation of China(No.20772068)the National Key Project of Scientific and Technical Supporting Programs of China(No.2006BAE01A01-5) for financial support
文摘Eleven new imine derivatives 6 containing 1H-1,2,4-triazole and thiazole rings were synthesized by the condensation of 5-((1H- 1,2,4-triazol-1-yl)methyl)-4-tert-butylthiazol-2-amine with various substituted benzaldehydes.The structures of the title compounds were characterized by ~1H NMR,MS and elemental analysis.The plant-growth regulatory activities of these compounds were evaluated.The primary bioassay results indicated that these target compounds exhibited promising plant-growth regulatory activities.
基金financial supported by the National Natural Science Foundation of China(No.21202089)China Postdoctoral Science Foundation(No.2013M531145)the Research Foundation of the Six People Peak of Jiangsu Province(No.2013-SWYY-013)
文摘A series of new pyrazole oximes bearing substituted thiazole ring were designed and prepared. The structures of the title compounds were identified by spectral analyses, The results of primary bioassay indicated that some targeted compounds exhibited promising insecticidal activity besides acaricidal activity, particularly; compounds 8c and 8d were more potent against Tetranychus cinnabarinus and Plutella xylostella than other analogues.
基金funded in part by the National Natural Science Foundation of China(21372132)NFFTBS(No.J1103306)
文摘The title compound 2-（1-（3-bromo-1-（3-chloropyridin-2-yl）-1H-pyrazole-5-carbonyl）piperidin-4-yl）-N-isopropylthiazole-4-carboxamide（C21H22Br Cl N6O2 S,Mr = 536.04） has been synthesized,and its structure was characterized by IR spectra,1H-NMR,13C-NMR,EA,and single-crystal X-ray diffraction.The crystal of the title compound belongs to monoclinic system,space group P/c with a = 15.146（3）,b = 11.573（2）,c = 26.937（5） A,β = 103.64（3）°,V = 1839.0（6） A^3,Z = 4,Dc = 1.557 g/cm^3,μ（Mo Ka） = 0.71073 mm^-1,F（000） = 2192,R = 0.0601 and w R = 0.1392.There exist one intramolecular hydrogen bond at N–H···N and four intermolecular weak interactions at O（2）···H（1）,Cl（1）···H（12）,O（1）···Cl（1） and S（1）···O（2）.Bioassay results indicated that the title compound had good fungicidal and antiviral activities against tobacco mosaic virus.
基金financial support provided by The National Key Research and Development Program of China (No. 2017YFD0200500)the National Natural Science Foundation of China (Nos. 21722202, 21672069, 21472050)+3 种基金S&TCSM of Shanghai (No. 18JC1415600),S&TCSM of Shanghai(No.18JC1415600)Fok Ying Tung Education Foundation(No. 141011)DFMEC(No. 20130076110023)Professor of Special Appointment(Eastern Scholar) at Shanghai Institutions of Higher Learning,National Program for Support of Top-Notch Young Professionals
文摘In recent decades, peptides as potential drugs were more and more explored with the development of non-oral medicine. There into, sulfur-containing peptide is one of the most popular aspects in peptide drugs due to the introduction of sulfur atoms leading unique properties.The purpose of the present review is to focus on the discovery of various sulfur-containing peptides with particular emphasis on their pharmacological mechanisms. This review is organized according to the structures of the sulfurcontaining peptides.
基金the Natural Science Foundation of University,Anhui Province(No.2006KJ156B)
文摘The title compound 2, 4-chloromethyl-3-anilino-2-（4-methyl-benzoylimido）thiazole, was prepared by the reaction of 1-p-methylbenzoyl-3-phenylaminothiourea 1 with 1,3-dichloro- acetone. The crystal is of monoclinic, space group P21/c, with a = 8.1712（15）, b = 10.998（2）, c = 19.134（4）A, β= 94.610（5）°, C18H16ClN3OS, Mr = 357.85, Z = 4, V = 1714.0（6）A^3, De= 1.387 g/cm^3, μ（MoKa） = 0.354 mm^-1, F（000） = 744, the final R = 0.0518 and wR = 0.1167 for 3189 observed reflections （I〉 2σ（I）. Its formation mechanism was proposed.
文摘A new kind of aromatic diamine monomer containing thiazole unit, 2-amino-5-（4-aminophenyl）-thiazole （AAPT）, was synthesized in three steps, starting from 4-nitroacetophenone. A novel thiazole-containing polyimide was prepared via the polycondensation of AAPT with 6FDA by one-step method. The resulting polyimide exhibits excellent solubility, film-forming capability and high thermal resistance.
文摘A series of new biquinoline derivatives containing a thiazole moiety were synthesized by a one-pot,base-catalyzed cyclocondensation reaction of 2-chloro-3-formyl quinoline,malononitrile and enaminone.All the synthesized compounds were characterized by elemental analysis,FT-IR,~1H NMR and ^（13）C NMR data.All the synthesized compounds were screened against three bacterial pathogens,namely Bacillus cereus,B.substilis and Escherichia coli and for antifungal activity against three fungal pathogens,Aspergillus niger,Fusarium oxisporum and Rhizopus using the disc diffusion method.
基金NFCRS,Nuclear Science&Technology Research Institute(Tehran,Iran)for their financial support
文摘A derivative of thiazole（AAT） has been explored as a sensing material for preparation a selective Lu（III） PVC-based membrane sensor.The proposed sensor exhibits a Nernstian response over a wide concentration range from 1.0×10^（-6） to 1.0×10^（-1） mol/L of Lu（Ⅲ） and the detection limit is 5.7×10^（-7） mol/L.The sensor response is independent of pH of the solution in the range 3.2-8.8 and possesses the advantages of fast response time（～6） and in particular,good selectivity to the lutetium ions with regard to most common metal ions,and especially all lanthanide ions.
基金supported by Dongguk University-Seoul,Republic of Korea,research funds 2016-2017supported by the KU Research Professor Program of Konkuk University, Seoul, Republic of Korea
文摘A new series of multi-heterocyclic Schiff base was constructed starting from 4＇-（imidazol-1-yl[56_TD$IF]）-acetophenone which was converted to its 2-bromoethanone precursor which on cyclic condensation with thiourea yielded final thiazol-2-amine intermediate（3） to be reacted with substituted aldehydes to generate final imidazolylphenylheterocyclic-2-ylmethylenethiazole-2-amines（4a–4i）. New Schiff base was investigated for their in vitro cytotoxic efficacies against a panel of three human cancer cell lines namely, MCF7（human breast cancer）, HCT116（human colon cancer）, and DU145（human prostate cancer） and one normal skin fibroblast（SF）. Most of these synthetic derivatives shown important cytotoxic actions against individual carcinoma cell line collections, but weak actions against SF, which is as anticipated. Observations of SAR suggested that the difference in the characteristics of substituents attached to the Schiff base function leads to the interesting variations within pharmacological effects of resultant molecular systems. Structural analysis performed using FT-IR,~1H NMR,^（13）C NMR spectroscopy and CHN analysis for final potent anticancer Schiff base, which warrant further investigations.
文摘The present work aimed to synthesize a new interesting series of thiazole based polyamides containing diarylidenecyclohexanone moiety 5a-5f using low temperature solution polycondensation technique. The new polymers were synthesized by the reaction of thiazole based monomer namely, bis（2-aminothiazol-4-ylbenzylidene）cyclohexanone 3 with different aliphatic and aromatic diacid chlorides using NMP, and in the presence of anhydrous Li Cl as catalyst. Adipoyl, sebacoyl, oxaloyl, terephthaloyl, isophthaloyl dichlorides and biphenyl dicarbonyl dichloride were used as diacid chlorides. The structure of the model compound 4 as well as the new polymers was confirmed by correct elemental and spectral analyses. The thermal properties of those polymers were evaluated by TGA and DTG measurements and correlated to their structural units, beside X-ray diffraction analysis, solubility and viscometry measurements. The inherent viscosities for the synthesized polymers were in the range 0.6–1.03 d L/g. On the other hand the corrosion inhibitive properties of monomer 3 as well as polyamides 5d and 5f as selected examples were carried out on carbon-steel in 0.5 mol/L H2SO4 at 40 °C. The calculated inhibition efficiency（IE%） for polymer 5d was in the range（82 ± 6）% in all selected concentrations. The best value of IE% was obtained at 1 mg/L to reach 98.24% for polymer 5d and at 0.5 mg/L to reach 87.75% for polymer 5f.
