Studies on structure-activity relationship of phenothiazines (PTZs) forinhibition of protein kinase C (PKC) and reversal of multidrug resistance (MDR) has been made invitro. The results showed that the order of potenc...Studies on structure-activity relationship of phenothiazines (PTZs) forinhibition of protein kinase C (PKC) and reversal of multidrug resistance (MDR) has been made invitro. The results showed that the order of potency of reversal effect of PTZs on MDR is as follows:2-COC_3 H_7 > 2-CF_3 > 2-COCH_3 > H. The type of piperazinyl substitution also significantlyaffected potency against MDR. The results show the order: CH_3 > COOC_2 H_5 > C_2 H_4 OH. Inaddition, PKC plays a marked role in diverse cellular process including MDR. Some derivatives of PTZwas tested for inhibition of PKC, of which PTZ11 showed the highest inhibitory effect of MDR andPKC, implying a potential reversal agent of MDR for tumor therapy in the future. We also tried toexplore the possible binding model of PTZs to PKC. Our molecular-modeling study preliminarilysuggests how these PTZs bind to PKC and provides a structural basis for the design of high affinityPKC-modulator. The infor-mation may be used in the rational design of more effective drugs.展开更多
A facile and elegant method for synthesis of novel N-aryl phenothiazine derivatives from 2-phenylindolizines and phenothiazines through direct electrochemical oxidation has been developed.This approach was performed s...A facile and elegant method for synthesis of novel N-aryl phenothiazine derivatives from 2-phenylindolizines and phenothiazines through direct electrochemical oxidation has been developed.This approach was performed smoothly at room temperature without external oxidant and catalyst.Cyclic voltammetry and in situ FTIR techniques were applied to analyze the cross-coupling process of phenothiazines and 2-phenylindolizines,which helped to select the appropriate reaction potential.Under the optimized conditions,a broad range of substrates were well tolerated,affording the desired products in moderate to excellent isolated yields(up to 91%)with high regioselectivity.Meanwhile,a plausible mechanism involving a radical pathway has been proposed.展开更多
The thermodynamic properties of 135 polychlorinated phenothiazines （PCPTZs） in the standard state are calculated using a combination of quantum mechanical computations performed with the Gaussian 03 program at the B...The thermodynamic properties of 135 polychlorinated phenothiazines （PCPTZs） in the standard state are calculated using a combination of quantum mechanical computations performed with the Gaussian 03 program at the B3LYP/6-311G^＊＊ level, and their octanol-water partition coefficients （logKow） are calculated based on group contributions. The chlorine substitution pattern strongly influenced the thermodynamic properties and hydrophilicity of the compounds. The thermodynamic properties of congeners also depend on the chlorine substitution pattern. The effect of chlorine substitution pattern is quantitatively studied by considering the mmaber and position of Cl atom substitution （Npcs）. The results show that the Npcs model may be used to predict the thermodynamic properties and hydrophilicity for all 135 PCPTZ congeners.展开更多
In the present study, actions of phenothiazines(PTZ) in reversing multidrug resistance(MDR) and inhibiting PKC activity were investigated. It was found that the three PTZs caused 2.49, 36.58 and 75.78 fold reversal of...In the present study, actions of phenothiazines(PTZ) in reversing multidrug resistance(MDR) and inhibiting PKC activity were investigated. It was found that the three PTZs caused 2.49, 36.58 and 75.78 fold reversal of K562/AO2 MDR cells resistant to adriamycin, respectively, while the chemosensitizer verapamil caused 40 fold reversal in the same condition, indicating that PTZ11 is a novel reversal agent of MDR and a potential chemotherapeutic reagent for tumor therapy. PKC activity analysis in the presence of PTZs showd that PTZ6 and PTZ11 inhibited rat brain protein kinase C activity in a manner of dose_dependent. The IC 50 values were (489.77±31.4) and (113±9.64) μmol/L, respectively. PTZ7 had no inhibition on PKC activity. Further study showed that PTZ11 could reduce PMA_mediated activation of PKC in a manner of dose_dependent, suggesting that PTZ11 might compete for the high_affinity phorbol ester binding site within PKC molecule. Recently, an X_ray structure of PMA in complex with PKC Cys2 activator_binding domain was solved. We therefore decided to explore the possible binding model of PTZ11 with PKC molecule using SYBYL 6.02 program. It was shown that the binding site of PTZ11 with PKC molecule partially overlapped with that of PMA, providing for the first time new data for designing PKC inhibitors and MDR reversal drugs.展开更多
Electron transfer reactions take place readily between 2, 2, 6, 6-tetramethylpiperidine oxoammonium ions (la,lb) and phenothiazines (2a—2g), giving corresponding nitroxides (3a,3b) and phenothiazine radical cations ...Electron transfer reactions take place readily between 2, 2, 6, 6-tetramethylpiperidine oxoammonium ions (la,lb) and phenothiazines (2a—2g), giving corresponding nitroxides (3a,3b) and phenothiazine radical cations (4a—4g). The rate constants for the electron self-exchange reactions between1 and3, as well as between2 and4, are determined by EPR and1HNMR line-broadening effect in acetonitrile. By application of the Marcus theory, the kinetics of the cross exchange reactions between1 and2 is studied.展开更多
U. V. irradiation of N-alkylphenothiazines (la—c) in carbon tetrachloride produced 3-(phenothiazin-N’-yl-carbonyl)-N’-alkylphenothiazine (2a—b) and/or 3-(N’-alkylphenothiazin-3’-yl-carbonyl) -N-alkylphenothiazin...U. V. irradiation of N-alkylphenothiazines (la—c) in carbon tetrachloride produced 3-(phenothiazin-N’-yl-carbonyl)-N’-alkylphenothiazine (2a—b) and/or 3-(N’-alkylphenothiazin-3’-yl-carbonyl) -N-alkylphenothiazine (3b—c) together with the radical cation carbon tetrachloride saltl +·CCl-· 4 (4a—c), presumably via a photoinduced electron transfer mechanism.展开更多
Three novel small-molecule donors(SMDs),namely PTZBT,PTZBBT and PTZSSBT,were designed and synthesized.Initially,a D-A-D type small molecule,PTZBT,was constructed using phenothiazine(PTZ)unit and benzothiadiazole(BT)un...Three novel small-molecule donors(SMDs),namely PTZBT,PTZBBT and PTZSSBT,were designed and synthesized.Initially,a D-A-D type small molecule,PTZBT,was constructed using phenothiazine(PTZ)unit and benzothiadiazole(BT)unit.To overcome the challenges posed by the high crystallinity and poor solubility of the BT structure,a 3D molecule,PTZBBT,was further developed by incorporating a 5,5'-biphenylthiadiazole(BBT)unit.It was demonstrated that the introduction of the BBT significantly enhanced the performance of photovoltaic devices.Subsequently,a D-π-A-π-D type 2D planar molecule,PTZSSBT,was synthesized by introducing bithiophene as theπ-bridge.This extended conjugated system not only enhances the planarity of the molecule but also broadens the absorption spectrum.Therefore,the devices based on PTZSSBT material device achieved excellent photovoltaic performance with a PCE of 4.38%and a J_(SC) of 13.51 mA·cm^(-2).This study highlights that the dual strategy of optimizing 3D configurations and extending 2D conjugation can synergistically enhance the performance of photovoltaic materials.展开更多
Purpose: Our practitioners are asked to consider a patient’s postoperative nausea and vomiting (PONV) risk profile when developing their prophylactic antiemetic strategy. There is wide variation in employed strategie...Purpose: Our practitioners are asked to consider a patient’s postoperative nausea and vomiting (PONV) risk profile when developing their prophylactic antiemetic strategy. There is wide variation in employed strategies, and we have yet to determine the most effective PONV prophylactic regimen. The objective of this study is to compare prophylactic antiemetic regimens containing: phenothiazines to 5HT3 antagonists for effectiveness at reducing the incidence of Post‐Anesthesia Care Unit (PACU) rescue antiemetic administration. Methods: This is an observational study of 4392 nonsmoking, women who underwent general anesthesia for breast surgery from 1/1/2009 through 6/30/2012. Previous history of PONV or motion sickness (HxPONV/MS) and the use of PACU opioids were recorded. Prophylactic antiemetic therapy was left to the discretion of the anesthesia care team. We compared phenothiazines and 5HT3 antagonists alone and with a glucocorticoid to determine the most effective treatment regimen in our practice for the prevention of the administration of PACU rescue antiemetics. Results: Patients who received a phenothiazine regimen compared to a 5HT3 antagonist regimen were less likely to have an antiemetic administered in the PACU (p = 0.0100) and this significant difference in rates holds in a logistic regression model adjusted for HxPONV/MS and PACU Opioid use (p = 0.0103). Conclusions: Based on our findings our clinicians are encouraged to administer a combination of a phenothiazine and a glucocorticoid in female, nonsmoking surgical breast patients for the prevention of PACU rescue antiemetic administration.展开更多
Chagas disease, caused by the protozoan Trypanosoma cruzi, is a relevant parasitic disease in the Americas. Current chemotherapy relies on Nifurtimox and Benznidazole, which present serious drawbacks, including high t...Chagas disease, caused by the protozoan Trypanosoma cruzi, is a relevant parasitic disease in the Americas. Current chemotherapy relies on Nifurtimox and Benznidazole, which present serious drawbacks, including high toxicity, low efficiency and the emergence of resistant strains. In the present work, the perspectives of levomepromazine, a tri-cyclic compound belonging to the family of phenotiazines with well-known properties as antipsychotics were evaluated as a potential anti-T. cruzi drug. We show that this drug is able to inhibit the proliferation of epimastigotes (IC50 = 0.41 ± 0.01 mM) and to interfere with the infection of the host cells (IC50 = 0.34 ± 0.01 mM). Interestingly, the treatment with levomepromazine affected the ability of metabolites such as glucose, proline and glutamate to fuel the recovery of epi-mastigotes after being submitted to metabolic stress. These findings prompt levomepromazine as a promising leader drug to obtain new trypanocidal activities.展开更多
Dye-sensitized solar cells（DSSCs） have attracted significant attention as alternatives to conventional silicon-based solar cells owing to their low-cost production,facile fabrication,excellent stability and high pow...Dye-sensitized solar cells（DSSCs） have attracted significant attention as alternatives to conventional silicon-based solar cells owing to their low-cost production,facile fabrication,excellent stability and high power conversion efficiency（PCE）.The dye molecule is one of the key components in DSSCs since it significant influence on the PCE,charge separation,light-harvesting,as well as the device stability.Among various dyes,easily tunable phenothiazine-based dyes hold a large proportion and achieve impressive photovoltaic performances.This class of dyes not only has superiorly non-planar butterfly structure but also possesses excellent electron donating ability and large π conjugated system.This review summarized recent developments in the phenothiazine dyes,including small molecule phenothiazine dyes,polymer phenothiazine dyes and phenothiazine dyes for co-sensitization,especially focused on the developments and design concepts of small molecule phenothiazine dyes,as well as the correlation between molecular structures and the photovoltaic performances.展开更多
Poly（pheniothiazine） films were prepared on a porous carbon felt（CF） electrode surface by an electrooxidative polymerization of three phenothiazine derivatives（i.e.,Tthionine（TN）,Toluidine Blue（TB） and Methyl...Poly（pheniothiazine） films were prepared on a porous carbon felt（CF） electrode surface by an electrooxidative polymerization of three phenothiazine derivatives（i.e.,Tthionine（TN）,Toluidine Blue（TB） and Methylene Blue（MB）） from 0.1 mol/L phosphate buffer solution（pH 7.0）.Among the three phenothiazies,the poly（TB） film-modified CF exhibited an excellent electrocatalytic activity for the oxidation of nicotinamide adenine dinucleotide reduced form（NADH） at ＋0.2 V vs.Ag/AgCl.The poly（TB） film-modified CF was successfully used as working electrode unit of highly sensitive amperometric flow-through detector for NADH.The peak currents（peak heights） were almost unchanged,irrespective of a carrier flow rate ranging from 2.0 to 4.1 mL/min,resulting in the measurement of NADH（ca.30 samples/hr） at 4.1 mL/min.The peak current responses of NADH showed linear relationship over the concentration range from 1 to 30 μmol/L（sensitivity：0.318 μA/（μmol/L）;correlation coefficient：0.997）.The lower detection limit was found to be 0.3 μmol/L（S/N = 3）.展开更多
Polymeric organic battery materials are promising alternatives to the transition-metal-based ones owing to their enriched chemistries. However, the flammability of organic compounds brings in serious concern on batter...Polymeric organic battery materials are promising alternatives to the transition-metal-based ones owing to their enriched chemistries. However, the flammability of organic compounds brings in serious concern on battery safety. In addition to use flame-retarding electrolyte/electrolyte additives or battery separators,flame retardancy can readily be achieved through the integration of flame-retarding unit into the polymer backbone, imparting the flame retardancy permanently. The as-designed polymer based on phenothiazine shows significantly shortened self-extinguished time without deteriorating its intrinsic thermodynamic and electrochemical properties. Moreover, two electron per phenothiazine molecule is realized for the first time in a highly reversible manner with discharge voltages of 3.52 V and 4.16 V versus Li+/Li and an average capacity of ca. 120 mAh g-1 at a current rate of 2 C. The origin of the reversibility is investigated through density functional theory(DFT) calculations. These findings address the importance of molecular design for safer and more stable organic materials for batteries.展开更多
The photo-induced electron transfer reactions of anthracene with N,N -diethylaniline(DEA) and phenothiazine(PTZ) occur in the membrane phase of a Triton X-100/ n -C 10 H 21 OH(1-decanol)/H 2O microemulsion. DEA and PT...The photo-induced electron transfer reactions of anthracene with N,N -diethylaniline(DEA) and phenothiazine(PTZ) occur in the membrane phase of a Triton X-100/ n -C 10 H 21 OH(1-decanol)/H 2O microemulsion. DEA and PTZ exist in the membrane phase of the microemulsion. Anthracene exists in the oil continuous phase of the W/O microemulsion and in the oil core and membrane phase of the O/W microemulsion.展开更多
he stable radical cation salts of phenothiazine and N-alkyl-phenothiazine(alkyl =methyl , ethyl , isohutyl , isopentyl and benzyl) hexachloroantimonate ,per-chlorate , and iodide were prepared by means of one-electron...he stable radical cation salts of phenothiazine and N-alkyl-phenothiazine(alkyl =methyl , ethyl , isohutyl , isopentyl and benzyl) hexachloroantimonate ,per-chlorate , and iodide were prepared by means of one-electron oxidation with 2 ,2 , 6 ,6-tetramethyl- 4-acetoxypiperidine oxoammonium hexachloroantimonate , perchloricacid, hydrogen peroxide, and molecular iodine, respectively. The radical cationswere characterized using ESR spectroscopy. Conformational analysis based on theESR parameters suggests that the radical cations adopt a planar configuration withthe nitrogen radical as the center.展开更多
Copolymers of fluorene-co-phenothiazine （ P1） and th iophene-co-phenothiazine （ P2 ） were prepared respectively by Wittig reaction. The synthesis, photo-physical and electroluminescent properties of the resulting ...Copolymers of fluorene-co-phenothiazine （ P1） and th iophene-co-phenothiazine （ P2 ） were prepared respectively by Wittig reaction. The synthesis, photo-physical and electroluminescent properties of the resulting polymers were analyzed by FT-IR, GPC, IH-NMR, UV-Vis, Photoluminescence （PL）, Electroluminescence （EL） and Cyclic Voltammetry （CV）. Their single layer devices with configuration of lTO/polymers/Ca/Al were studied. GPC results revealed the weight-average molecular weight （Mw） was 3.0×10^3 and 5.4×10^3, respectively. The device with a single layer structure of ITO/P1/Ca/Al emits green light with the maximum peak at 552nm. However, the device with a single layer structure of ITO/P2/Ca/Al emit red light with the maximum peak at 616nm.展开更多
A new ligand, 10ethylphenothiazinyl 3 yl methylene thiosemicarbazon (HL) and its complexes ML2 (M=Zn2+, Cd2+), which exhibit intensive two-photon excited (TPE) fluorescence at 800 nm laser pulses in femtosecond reg...A new ligand, 10ethylphenothiazinyl 3 yl methylene thiosemicarbazon (HL) and its complexes ML2 (M=Zn2+, Cd2+), which exhibit intensive two-photon excited (TPE) fluorescence at 800 nm laser pulses in femtosecond regime, were synthesized and characterized. The measured power dependence of the fluorescence signals provided direct evidence for TPE. All of them exhibited a large two-photon absorptive cross section and, more importantly from the application point of view, high photochemical/photothermal stability.展开更多
The interaction between amphiphilic porphyrin and phenothiazine in AOT/isooctane/water reverse micelle was investigated by UV-Vis spectra. A new absorption complex between the two species is formed in such circumstanc...The interaction between amphiphilic porphyrin and phenothiazine in AOT/isooctane/water reverse micelle was investigated by UV-Vis spectra. A new absorption complex between the two species is formed in such circumstances, which is ascribed to the enrichment of the components by the reverse micelle. The fluorescence quenching of CHTTP by PTH becomes more efficient after the formation of the absorption complex.展开更多
Macrocycle confinement induced vip near-infrared(NIR)luminescence was research hotspot currently.Here in,we reported a cucurbit[7]uril(CB[7])confined 3,7-bis((E)-2-(pyridin-4-yl)vinyl)-10-Hphenothiazine bridged bis(...Macrocycle confinement induced vip near-infrared(NIR)luminescence was research hotspot currently.Here in,we reported a cucurbit[7]uril(CB[7])confined 3,7-bis((E)-2-(pyridin-4-yl)vinyl)-10-Hphenothiazine bridged bis(4-(4-bromophenyl)pyridine)(G),which not only boosted its NIR luminescence but also realized detection of HClO/ClO^(-)in living cells and lysosome imaging.Fluorescence spectroscopy experiments were performed to calculate the detection ability of probe G to HClO/ClO^(-)up to 147 nmol/L.As compared with G,supramolecular probe G■CB[7]formed after encapsulated by CB[7],the detection ability towards HClO/ClO^(-)was improved to 24 nmol/L which was ascribe to the macrocycle CB[7]confinement increasing the fluorescence intensity to 103 folds.Accompanying the excitation wavelength changing,the fluorescence red-shifted to 820 nm when excited by 570 nm light,which was used to NIR lysosome imaging.Meanwhile,the supramolecular assembly G■CB[7]was also successfully used to highly sense to exogenous HClO/ClO^(-)in RAW 264.7 cells and live animal.展开更多
Inclusion of Acyclodextrin (ACD) with phenothiazine 1 and Nalkylpheno-thiazine derivatives (alkyl = ethyl 2, isobutyl 3 and isopentyl 4) in aqueous solution was studied by means of UV-vis spectroscopy. The association...Inclusion of Acyclodextrin (ACD) with phenothiazine 1 and Nalkylpheno-thiazine derivatives (alkyl = ethyl 2, isobutyl 3 and isopentyl 4) in aqueous solution was studied by means of UV-vis spectroscopy. The association constant Ka values for the inclusion of β-CD with 1, 2, 3 and 4 were determined to be 188, 214, 129 and 80 L/mol, respectively. It indicates that the stability of the inclusion complexes is dependent on the structure and the volume of the substituents in the vip compounds.展开更多
Photo-responsive room-temperature phosphorescent(RTP)materials have garnered significant interest due to the advantages of rapid response,spatiotemporal control,and contactless precision manipulation.However,the devel...Photo-responsive room-temperature phosphorescent(RTP)materials have garnered significant interest due to the advantages of rapid response,spatiotemporal control,and contactless precision manipulation.However,the development of such materials remains in its infancy,underscoring the importance of exploiting novel and efficient light-responsive RTP molecules.In this work,three phenothiazine derivatives of TPA-PTZ,TPA-2PTZ,and TPA-3PTZ were successfully synthesized via the Buchwald-Hartwig C—N coupling reaction.By embedding these molecules as RTP vips into polymethyl methacrylate(PMMA)matrix,photo-induced RTP properties were realized.Upon sustained UV irradiation,there was an enhancement of 19 times in the quantum yield to reach a value of 5.68%.Remarkably,these materials exhibit superior alongside robust light and thermal stability,maintaining high phosphorescence intensity even after prolonged UV exposure(irradiation for>200 s by a 365 nm UV lamp with the power of 500μW·cm-2)or at higher temperature up to 75℃.The outstanding properties of these photo-induced RTP materials make them promising candidates for applications in information encryption,anti-counterfeiting,and advanced optical materials.展开更多
文摘Studies on structure-activity relationship of phenothiazines (PTZs) forinhibition of protein kinase C (PKC) and reversal of multidrug resistance (MDR) has been made invitro. The results showed that the order of potency of reversal effect of PTZs on MDR is as follows:2-COC_3 H_7 > 2-CF_3 > 2-COCH_3 > H. The type of piperazinyl substitution also significantlyaffected potency against MDR. The results show the order: CH_3 > COOC_2 H_5 > C_2 H_4 OH. Inaddition, PKC plays a marked role in diverse cellular process including MDR. Some derivatives of PTZwas tested for inhibition of PKC, of which PTZ11 showed the highest inhibitory effect of MDR andPKC, implying a potential reversal agent of MDR for tumor therapy in the future. We also tried toexplore the possible binding model of PTZs to PKC. Our molecular-modeling study preliminarilysuggests how these PTZs bind to PKC and provides a structural basis for the design of high affinityPKC-modulator. The infor-mation may be used in the rational design of more effective drugs.
基金the generous financial support of the National Natural Science Foundations of China(Nos.22178321,21773211 and 21776260)。
文摘A facile and elegant method for synthesis of novel N-aryl phenothiazine derivatives from 2-phenylindolizines and phenothiazines through direct electrochemical oxidation has been developed.This approach was performed smoothly at room temperature without external oxidant and catalyst.Cyclic voltammetry and in situ FTIR techniques were applied to analyze the cross-coupling process of phenothiazines and 2-phenylindolizines,which helped to select the appropriate reaction potential.Under the optimized conditions,a broad range of substrates were well tolerated,affording the desired products in moderate to excellent isolated yields(up to 91%)with high regioselectivity.Meanwhile,a plausible mechanism involving a radical pathway has been proposed.
文摘The thermodynamic properties of 135 polychlorinated phenothiazines （PCPTZs） in the standard state are calculated using a combination of quantum mechanical computations performed with the Gaussian 03 program at the B3LYP/6-311G^＊＊ level, and their octanol-water partition coefficients （logKow） are calculated based on group contributions. The chlorine substitution pattern strongly influenced the thermodynamic properties and hydrophilicity of the compounds. The thermodynamic properties of congeners also depend on the chlorine substitution pattern. The effect of chlorine substitution pattern is quantitatively studied by considering the mmaber and position of Cl atom substitution （Npcs）. The results show that the Npcs model may be used to predict the thermodynamic properties and hydrophilicity for all 135 PCPTZ congeners.
文摘In the present study, actions of phenothiazines(PTZ) in reversing multidrug resistance(MDR) and inhibiting PKC activity were investigated. It was found that the three PTZs caused 2.49, 36.58 and 75.78 fold reversal of K562/AO2 MDR cells resistant to adriamycin, respectively, while the chemosensitizer verapamil caused 40 fold reversal in the same condition, indicating that PTZ11 is a novel reversal agent of MDR and a potential chemotherapeutic reagent for tumor therapy. PKC activity analysis in the presence of PTZs showd that PTZ6 and PTZ11 inhibited rat brain protein kinase C activity in a manner of dose_dependent. The IC 50 values were (489.77±31.4) and (113±9.64) μmol/L, respectively. PTZ7 had no inhibition on PKC activity. Further study showed that PTZ11 could reduce PMA_mediated activation of PKC in a manner of dose_dependent, suggesting that PTZ11 might compete for the high_affinity phorbol ester binding site within PKC molecule. Recently, an X_ray structure of PMA in complex with PKC Cys2 activator_binding domain was solved. We therefore decided to explore the possible binding model of PTZ11 with PKC molecule using SYBYL 6.02 program. It was shown that the binding site of PTZ11 with PKC molecule partially overlapped with that of PMA, providing for the first time new data for designing PKC inhibitors and MDR reversal drugs.
基金Project supported by the National Natural Science Foundation of China (Grant No. 29572047)
文摘Electron transfer reactions take place readily between 2, 2, 6, 6-tetramethylpiperidine oxoammonium ions (la,lb) and phenothiazines (2a—2g), giving corresponding nitroxides (3a,3b) and phenothiazine radical cations (4a—4g). The rate constants for the electron self-exchange reactions between1 and3, as well as between2 and4, are determined by EPR and1HNMR line-broadening effect in acetonitrile. By application of the Marcus theory, the kinetics of the cross exchange reactions between1 and2 is studied.
基金Project supported by the National Natural Science Foundation of China (Grant No. 29572047)the State Education Commission of China (Grant No. 9473001)
文摘U. V. irradiation of N-alkylphenothiazines (la—c) in carbon tetrachloride produced 3-(phenothiazin-N’-yl-carbonyl)-N’-alkylphenothiazine (2a—b) and/or 3-(N’-alkylphenothiazin-3’-yl-carbonyl) -N-alkylphenothiazine (3b—c) together with the radical cation carbon tetrachloride saltl +·CCl-· 4 (4a—c), presumably via a photoinduced electron transfer mechanism.
基金supported by the National Natural Science Foundation of China(21102013)the Fundamental Research Funds for the Central Universities(DUT16ZD205)
文摘Three novel small-molecule donors(SMDs),namely PTZBT,PTZBBT and PTZSSBT,were designed and synthesized.Initially,a D-A-D type small molecule,PTZBT,was constructed using phenothiazine(PTZ)unit and benzothiadiazole(BT)unit.To overcome the challenges posed by the high crystallinity and poor solubility of the BT structure,a 3D molecule,PTZBBT,was further developed by incorporating a 5,5'-biphenylthiadiazole(BBT)unit.It was demonstrated that the introduction of the BBT significantly enhanced the performance of photovoltaic devices.Subsequently,a D-π-A-π-D type 2D planar molecule,PTZSSBT,was synthesized by introducing bithiophene as theπ-bridge.This extended conjugated system not only enhances the planarity of the molecule but also broadens the absorption spectrum.Therefore,the devices based on PTZSSBT material device achieved excellent photovoltaic performance with a PCE of 4.38%and a J_(SC) of 13.51 mA·cm^(-2).This study highlights that the dual strategy of optimizing 3D configurations and extending 2D conjugation can synergistically enhance the performance of photovoltaic materials.
文摘Purpose: Our practitioners are asked to consider a patient’s postoperative nausea and vomiting (PONV) risk profile when developing their prophylactic antiemetic strategy. There is wide variation in employed strategies, and we have yet to determine the most effective PONV prophylactic regimen. The objective of this study is to compare prophylactic antiemetic regimens containing: phenothiazines to 5HT3 antagonists for effectiveness at reducing the incidence of Post‐Anesthesia Care Unit (PACU) rescue antiemetic administration. Methods: This is an observational study of 4392 nonsmoking, women who underwent general anesthesia for breast surgery from 1/1/2009 through 6/30/2012. Previous history of PONV or motion sickness (HxPONV/MS) and the use of PACU opioids were recorded. Prophylactic antiemetic therapy was left to the discretion of the anesthesia care team. We compared phenothiazines and 5HT3 antagonists alone and with a glucocorticoid to determine the most effective treatment regimen in our practice for the prevention of the administration of PACU rescue antiemetics. Results: Patients who received a phenothiazine regimen compared to a 5HT3 antagonist regimen were less likely to have an antiemetic administered in the PACU (p = 0.0100) and this significant difference in rates holds in a logistic regression model adjusted for HxPONV/MS and PACU Opioid use (p = 0.0103). Conclusions: Based on our findings our clinicians are encouraged to administer a combination of a phenothiazine and a glucocorticoid in female, nonsmoking surgical breast patients for the prevention of PACU rescue antiemetic administration.
基金supported by grants from the Fundacao de Amparo a Pesquisa do Estado de Sao Paulo(FAPESP grant#11/50631-1 to AMS),Instituto Nacional de Biologia Estrutural e Química Medicinal em Doencas Infecciosas(INBEQMeDI)Conselho Nacional de Desenvolvimento Científico e Tecnológico(CNPq grant#470272/2011-2 to AMS).
文摘Chagas disease, caused by the protozoan Trypanosoma cruzi, is a relevant parasitic disease in the Americas. Current chemotherapy relies on Nifurtimox and Benznidazole, which present serious drawbacks, including high toxicity, low efficiency and the emergence of resistant strains. In the present work, the perspectives of levomepromazine, a tri-cyclic compound belonging to the family of phenotiazines with well-known properties as antipsychotics were evaluated as a potential anti-T. cruzi drug. We show that this drug is able to inhibit the proliferation of epimastigotes (IC50 = 0.41 ± 0.01 mM) and to interfere with the infection of the host cells (IC50 = 0.34 ± 0.01 mM). Interestingly, the treatment with levomepromazine affected the ability of metabolites such as glucose, proline and glutamate to fuel the recovery of epi-mastigotes after being submitted to metabolic stress. These findings prompt levomepromazine as a promising leader drug to obtain new trypanocidal activities.
基金the National Natural Science Foundation of China(Nos.21572030,21272033,21402023)Fundamental Research Funds for the Central Universities(No.ZYGX2014J026)for financial support
文摘Dye-sensitized solar cells（DSSCs） have attracted significant attention as alternatives to conventional silicon-based solar cells owing to their low-cost production,facile fabrication,excellent stability and high power conversion efficiency（PCE）.The dye molecule is one of the key components in DSSCs since it significant influence on the PCE,charge separation,light-harvesting,as well as the device stability.Among various dyes,easily tunable phenothiazine-based dyes hold a large proportion and achieve impressive photovoltaic performances.This class of dyes not only has superiorly non-planar butterfly structure but also possesses excellent electron donating ability and large π conjugated system.This review summarized recent developments in the phenothiazine dyes,including small molecule phenothiazine dyes,polymer phenothiazine dyes and phenothiazine dyes for co-sensitization,especially focused on the developments and design concepts of small molecule phenothiazine dyes,as well as the correlation between molecular structures and the photovoltaic performances.
基金financially supported in part by the Open Research Center Project of the Ministry of Education,Science and Culture of Japan
文摘Poly（pheniothiazine） films were prepared on a porous carbon felt（CF） electrode surface by an electrooxidative polymerization of three phenothiazine derivatives（i.e.,Tthionine（TN）,Toluidine Blue（TB） and Methylene Blue（MB）） from 0.1 mol/L phosphate buffer solution（pH 7.0）.Among the three phenothiazies,the poly（TB） film-modified CF exhibited an excellent electrocatalytic activity for the oxidation of nicotinamide adenine dinucleotide reduced form（NADH） at ＋0.2 V vs.Ag/AgCl.The poly（TB） film-modified CF was successfully used as working electrode unit of highly sensitive amperometric flow-through detector for NADH.The peak currents（peak heights） were almost unchanged,irrespective of a carrier flow rate ranging from 2.0 to 4.1 mL/min,resulting in the measurement of NADH（ca.30 samples/hr） at 4.1 mL/min.The peak current responses of NADH showed linear relationship over the concentration range from 1 to 30 μmol/L（sensitivity：0.318 μA/（μmol/L）;correlation coefficient：0.997）.The lower detection limit was found to be 0.3 μmol/L（S/N = 3）.
基金financial support from the National Natural Science Foundation of China (grant no.51772199)the Natural Science Foundation of Jiangsu Province (Grant no.BK20170329)+2 种基金the Collaborative Innovation Center of Suzhou Nano Science & Technologythe Priority Academic Program Development of Jiangsu Higher Education Institutionsthe 111 Project。
文摘Polymeric organic battery materials are promising alternatives to the transition-metal-based ones owing to their enriched chemistries. However, the flammability of organic compounds brings in serious concern on battery safety. In addition to use flame-retarding electrolyte/electrolyte additives or battery separators,flame retardancy can readily be achieved through the integration of flame-retarding unit into the polymer backbone, imparting the flame retardancy permanently. The as-designed polymer based on phenothiazine shows significantly shortened self-extinguished time without deteriorating its intrinsic thermodynamic and electrochemical properties. Moreover, two electron per phenothiazine molecule is realized for the first time in a highly reversible manner with discharge voltages of 3.52 V and 4.16 V versus Li+/Li and an average capacity of ca. 120 mAh g-1 at a current rate of 2 C. The origin of the reversibility is investigated through density functional theory(DFT) calculations. These findings address the importance of molecular design for safer and more stable organic materials for batteries.
基金Supported by the National Natural Science Foundation of China( No.2 0 0 730 38,2 0 2 330 10 )
文摘The photo-induced electron transfer reactions of anthracene with N,N -diethylaniline(DEA) and phenothiazine(PTZ) occur in the membrane phase of a Triton X-100/ n -C 10 H 21 OH(1-decanol)/H 2O microemulsion. DEA and PTZ exist in the membrane phase of the microemulsion. Anthracene exists in the oil continuous phase of the W/O microemulsion and in the oil core and membrane phase of the O/W microemulsion.
文摘he stable radical cation salts of phenothiazine and N-alkyl-phenothiazine(alkyl =methyl , ethyl , isohutyl , isopentyl and benzyl) hexachloroantimonate ,per-chlorate , and iodide were prepared by means of one-electron oxidation with 2 ,2 , 6 ,6-tetramethyl- 4-acetoxypiperidine oxoammonium hexachloroantimonate , perchloricacid, hydrogen peroxide, and molecular iodine, respectively. The radical cationswere characterized using ESR spectroscopy. Conformational analysis based on theESR parameters suggests that the radical cations adopt a planar configuration withthe nitrogen radical as the center.
基金Tianjin Natural Sci. Found. (033800311) Key Project of Chinese Ministry of Education (205007)+2 种基金 Sci. Develop. Found. of Tianjin Education Commission (20030426, 20041017, 20050520) the German Federal Ministry for Education and Research (BMBF, CHN 05/011) the National Nature Sci. Found. (60276027) and Tianjin Key Discipline of Mat. Phy. and Chem.
文摘Copolymers of fluorene-co-phenothiazine （ P1） and th iophene-co-phenothiazine （ P2 ） were prepared respectively by Wittig reaction. The synthesis, photo-physical and electroluminescent properties of the resulting polymers were analyzed by FT-IR, GPC, IH-NMR, UV-Vis, Photoluminescence （PL）, Electroluminescence （EL） and Cyclic Voltammetry （CV）. Their single layer devices with configuration of lTO/polymers/Ca/Al were studied. GPC results revealed the weight-average molecular weight （Mw） was 3.0×10^3 and 5.4×10^3, respectively. The device with a single layer structure of ITO/P1/Ca/Al emits green light with the maximum peak at 552nm. However, the device with a single layer structure of ITO/P2/Ca/Al emit red light with the maximum peak at 616nm.
基金This work was supported by the grant for the State Key Program of China(G1998061402)the National Natural Science Foundation of China(29871001,20071001).
文摘A new ligand, 10ethylphenothiazinyl 3 yl methylene thiosemicarbazon (HL) and its complexes ML2 (M=Zn2+, Cd2+), which exhibit intensive two-photon excited (TPE) fluorescence at 800 nm laser pulses in femtosecond regime, were synthesized and characterized. The measured power dependence of the fluorescence signals provided direct evidence for TPE. All of them exhibited a large two-photon absorptive cross section and, more importantly from the application point of view, high photochemical/photothermal stability.
基金We thank the National Natural Science Foundation of China,the Ministry of ScienceTechnology of China(grant No.29971031,20073050,and G2000028204)for financial support.
文摘The interaction between amphiphilic porphyrin and phenothiazine in AOT/isooctane/water reverse micelle was investigated by UV-Vis spectra. A new absorption complex between the two species is formed in such circumstances, which is ascribed to the enrichment of the components by the reverse micelle. The fluorescence quenching of CHTTP by PTH becomes more efficient after the formation of the absorption complex.
基金financially supported by the National Natural Science Foundation of China(No.22131008)Liaocheng University Start-up Fund for Doctoral Scientific Research(No.318052327)。
文摘Macrocycle confinement induced vip near-infrared(NIR)luminescence was research hotspot currently.Here in,we reported a cucurbit[7]uril(CB[7])confined 3,7-bis((E)-2-(pyridin-4-yl)vinyl)-10-Hphenothiazine bridged bis(4-(4-bromophenyl)pyridine)(G),which not only boosted its NIR luminescence but also realized detection of HClO/ClO^(-)in living cells and lysosome imaging.Fluorescence spectroscopy experiments were performed to calculate the detection ability of probe G to HClO/ClO^(-)up to 147 nmol/L.As compared with G,supramolecular probe G■CB[7]formed after encapsulated by CB[7],the detection ability towards HClO/ClO^(-)was improved to 24 nmol/L which was ascribe to the macrocycle CB[7]confinement increasing the fluorescence intensity to 103 folds.Accompanying the excitation wavelength changing,the fluorescence red-shifted to 820 nm when excited by 570 nm light,which was used to NIR lysosome imaging.Meanwhile,the supramolecular assembly G■CB[7]was also successfully used to highly sense to exogenous HClO/ClO^(-)in RAW 264.7 cells and live animal.
文摘Inclusion of Acyclodextrin (ACD) with phenothiazine 1 and Nalkylpheno-thiazine derivatives (alkyl = ethyl 2, isobutyl 3 and isopentyl 4) in aqueous solution was studied by means of UV-vis spectroscopy. The association constant Ka values for the inclusion of β-CD with 1, 2, 3 and 4 were determined to be 188, 214, 129 and 80 L/mol, respectively. It indicates that the stability of the inclusion complexes is dependent on the structure and the volume of the substituents in the vip compounds.
文摘Photo-responsive room-temperature phosphorescent(RTP)materials have garnered significant interest due to the advantages of rapid response,spatiotemporal control,and contactless precision manipulation.However,the development of such materials remains in its infancy,underscoring the importance of exploiting novel and efficient light-responsive RTP molecules.In this work,three phenothiazine derivatives of TPA-PTZ,TPA-2PTZ,and TPA-3PTZ were successfully synthesized via the Buchwald-Hartwig C—N coupling reaction.By embedding these molecules as RTP vips into polymethyl methacrylate(PMMA)matrix,photo-induced RTP properties were realized.Upon sustained UV irradiation,there was an enhancement of 19 times in the quantum yield to reach a value of 5.68%.Remarkably,these materials exhibit superior alongside robust light and thermal stability,maintaining high phosphorescence intensity even after prolonged UV exposure(irradiation for>200 s by a 365 nm UV lamp with the power of 500μW·cm-2)or at higher temperature up to 75℃.The outstanding properties of these photo-induced RTP materials make them promising candidates for applications in information encryption,anti-counterfeiting,and advanced optical materials.
