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Science China Chemistry 2014年第6期57卷 807-822页

作者： ZHANG HuiZhen LIN JianMei RASHEED Syed zhou chenghe School of Chemistry and Chemical Engineering Southwest University Sichuan Provincial People's Hospital

A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS *** the new compounds were screened for their antimicrobial activities in vitro by a twofold serial dilution *** bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles were comparably or even more strongly antibacterial and antifungal than the reference drugs Chloromycin,Norfloxacin,and *** combination of2,4-difluorobenzyl benzimidazole derivative 5l and its hydrochloride 7 respectively with the antibacterials Chloromycin,Norfloxacin,and the antifungal Fluconazole was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive *** addition,the interaction of compound 5l with calf thymus DNA demonstrated that this compound could effectively intercalate into DNA to form a compound 5l-DNA complex that might block DNA replication and thereby exert good antimicrobial activity.

关键词： benzimidazole antibacterial antifungal calf thymus DNA synergistic effect

Review on supermolecules as chemical drugs

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Science China Chemistry 2009年第4期52卷 415-458页

作者： zhou chenghe GAN LinLing ZHANG YiYi ZHANG FeiFei WANG Guangzhou JIN Lei GENG RongXia School of Chemistry and Chemical Engineering Southwest UniversityChongqing 400715China School of Pharmaceutical Sciences Southwest UniversityChongqing 400715China

Supramolecular medicinal chemistry field has been a quite rapidly developing,increasingly active and newly rising interdiscipline which is the new expansion of supramolecular chemistry in pharmaceu-tical sciences,and is gradually becoming a relatively independent scientific area. Supramolecular drugs could be defined as medicinal supermolecules formed by two or more molecules through non-covalent bonds. So far a lot of supermolecules as chemical drugs have been widely used in clinics. Supermolecules as chemical drugs,i.e. supramolecular chemical drugs or supramolecular drugs,which might have the excellences of lower cost,shorter period,higher potential as clinical drugs for their successful research and development,may possess higher bioavailability,better biocompatibility and drug-targeting,fewer multidrug-resistances,lower toxicity,less adverse effect,and better curative effects as well as safety,and therefore exhibit wide potential application. These overwhelming advan-tages have drawn enormous special attention. This paper gives the definition of supramolecular drugs,proposes the concept of supramolecular chemical drugs,and systematically reviews the recent ad-vances in the research and development of supermolecules,including organic and inorganic complex ones as chemical drugs in the area of antitumor,anti-inflammatory,analgesic,antimalarial,antibacterial,antifungal,antivirus,anti-epileptic,cardiovascular agents and magnetic resonance imaging agents and so on. The perspectives of the foreseeable future and potential application of supramolecules as chemical drugs are also presented.

关键词： supramolecular chemistry cyclodextrin porphyrin complex anticancer anti-inflammatory antibacterial antifungal antivirus cardiovascular agent magnetic resonance imaging agent supramolecular drug

Chalcone-Benzotriazole Conjugates as New Potential Antimicrobial Agents： Design, Synthesis, Biological Evaluation and Synergism with Clinical Drugs

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Chinese Journal of Chemistry 2017年第4期35卷 483-496页

作者： Hanbo Liu Lavanya Gopala Srinivasa Rao Avula Ponmani Jeyakkumar Xinmei Peng chenghe zhou Rongxia Geng Institute of Bioorganic & Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing Municipality School of Chemistry and Chemical Engineering Southwest University Chongqing 400715 China School of Chemistry and Chemical Engineering Qiannan Normal University for Nationalities Duyun Guizhou 558000 China

A series of chalcone-benzotriazole conjugates as new potential antimicrobial agents were synthesized and char- acterized by ^1H NMR, ^13C NMR, IR and HRMS spectra. Antimicrobial assay manifested that some target com- pounds gave moderate to good antibacterial and antifungal activities. The N- 1 derived benzotriazole 5e and N-2 de- rived benzotriazole 6a exhibited valuable inhibitory efficacy against some tested strains. Especially, derivative 6a gave superior antifungal efficacies against C. utilis, S. cerevisiae and A. flavus （MIC^0.01, 0.02, 0.02 gmol/mL, respectively） to Fluconazole. The drug combination of compound 5e or 6a with antibacterial Chloromycin, Nor- floxacin and antifungal Fluconazole respectively showed stronger antimicrobial efficiency with less dosage and broader antimicrobial spectrum than their separated use alone. The preliminary interaction with calf thymus DNA revealed that compound 6a could intercalate into DNA to form 6a-DNA supramolecular complex which might be a factor to exert its powerful bioactivity. Molecular docking study indicated strong binding of compound 6a with DNA gyrase. The structural parameters such as molecular orbital energy and molecular electrostatic potential of compound 6a were also investigated, which provided better understanding for its good antimicrobial activity.

关键词： chalcone benzotriazole antimicrobial calf thymus DNA DNA gyrase

A series of naphthalimide azoles: Design, synthesis and bioactive evaluation as potential antimicrobial agents

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Science China Chemistry 2013年第7期56卷 952-969页

作者： DAMU Guri L. V. WANG QingPeng ZHANG HuiZhen ZHANG YiYi LV JingSong zhou chenghe School of Chemistry and Chemical Engineering Southwest University School of Chemistry and Chemical Engineering Bijie University

A series of naphthalimide azoles as potential antibacterial and antifungal agents were conveniently and efficiently synthesized starting from commercially available 6-bromobenzo[de]isochromene-l,3-dione. All the new compounds were characterized by NMR, IR, MS and HRMS spectra. Their antimicrobial activities were evaluated against four Gram-positive bacteria, four Gram-negative bacteria and two fungi using two-fold serial dilution technique. The biological assay indicated that most of the prepared compounds exhibited inhibition to the tested strains. In particular, the triazolium derivatives not only gave higher ef- ficacy than their corresponding precursory azoles, but also demonstrated comparable or even better potency than the reference drugs Chloromycin, Orbifloxacin and Fluconazole. Some factors including structural fragments, pH and ClogP values of the target molecules were also preliminarily discussed.

关键词： naphthalimide triazole imidazole triazolium imidazolium thiol thione antibacterial antifungal antimicrobial

Synthesis and biological activities of thio-triazole derivatives as novel potential antibacterial and antifungal agents

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Science China Chemistry 2012年第10期55卷 2134-2153页

作者： WANG QingPeng ZHANG JingQing DAMU Guri L.V. WAN Kun ZHANG HuiZhen zhou chenghe School of Chemistry and Chemical Engineering Southwest UniversityChongqing 400715China Chongqing Key Laboratory of Biochemical&Molecular Pharmacology Medicine Engineering Research CenterChongqing Medical UniversityChongqing 400016China

A series of novel thio-triazole derivatives including thiols, thioethers and thiones as well as some corresponding triazolium compounds were conveniently and efficiently synthesized from commercially available halobenzyl halides and thiosemicarbazide. All the new compounds were characterized by 1 H NMR, 13 C NMR, FTIR, MS and HRMS spectra. Their antibacterial and antifungal activities in vitro were evaluated against four Gram-positive bacteria, four Gram-negative bacteria and two fungi by two-fold serial dilution technique. The preliminary bioassay indicated that some prepared triazoles exhibited effective antibacterial and antifungal activities. Especially, 3,4-dichlorobenzyl triazolethione and its triazolium derivatives displayed the most potent activities against all the tested strains.

关键词： triazole triazolium antibacterial antifungal cyclization

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地西泮与乙醇协同作用机制的荧光光谱分析

高等学校化学学报 2018年第6期39卷 1178-1184页

作者：崔胜峰万敬伟周成合铁道警察学院公安技术系理化物证检验研究中心郑州450053 西南大学化学化工学院重庆市高校应用化学重点实验室重庆400715

基于荧光光谱分析技术,通过体外模拟生理环境实验和动物体内实验探索了地西泮与乙醇的协同作用机制.研究结果表明,在地西泮体内代谢初期,血液中乙醇的存在可以降低地西泮-人血清白蛋白(HSA)络合物的结合平衡常数,致使血液中地西泮游离... 详细信息

基于荧光光谱分析技术,通过体外模拟生理环境实验和动物体内实验探索了地西泮与乙醇的协同作用机制.研究结果表明,在地西泮体内代谢初期,血液中乙醇的存在可以降低地西泮-人血清白蛋白(HSA)络合物的结合平衡常数,致使血液中地西泮游离分子的浓度相对增大,可加速地西泮分子的代谢速率,降低药物的半衰期,从而增强地西泮在体内的药效,产生协同作用.

关键词：地西泮酒精依赖荧光光谱人血清白蛋白光谱分析

Synthesis,Antibacterial and Antifungal Activities of some New Coumarin Imidazole Derivatives

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Synthesis,Antibacterial and Antifungal Activities of some Ne...

有机合成创新—产业化的新动力——中国化学会全国第三届有机合成化学与过程学术讨论会

作者： Shi,Yuan zhou,chenghe~* (School of Chemistry and Chemical Engineering,Southwest University,Chongqing 400715)

A series of coumarin-based imidazole compounds were successfully synthesized starting from commercially available resorcin and were characterized by H NMR,C NMR MS and IR *** antimicrobial results exhibited that all target compounds gave more potential antimicrobial efficacy towards all tested microorganisms including methicillin-resistant *** and Fluconazole-insensitive ***,in comparison with currently antimicrobial drugs Enoaxin,Chloromycin and Fluconazole.

关键词： coumarin imidazoel antibacterial antifungal

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唑类超分子药物研究与应用

有机化学 2016年第1期36卷 1-42页

作者：程宇王辉 Dinesh Addla 周成合西南大学化学化工学院生物有机与药物化学研究所重庆市高校应用化学重点实验室重庆400715

基于非共价键力的超分子化学发展非常迅猛,在化学、物理、材料科学、信息科学以及医药等领域显示出广泛的应用前景和巨大的开发价值.唑类化合物如咪唑、噻唑、噁唑、吡唑、三唑、四唑和咔唑等具有特殊的含氮芳杂环结构,可通过非共价键... 详细信息

基于非共价键力的超分子化学发展非常迅猛,在化学、物理、材料科学、信息科学以及医药等领域显示出广泛的应用前景和巨大的开发价值.唑类化合物如咪唑、噻唑、噁唑、吡唑、三唑、四唑和咔唑等具有特殊的含氮芳杂环结构,可通过非共价键力与无机物和/或有机物形成络合物超分子,表现出广泛的生物活性.近些年来,唑类超分子在医药领域发展迅速,已成为研究热点领域之一.结合本课题组相关研究工作,参考国内外近五年文献,系统地综述了唑类超分子作为药物在抗癌、抗细菌、抗真菌、杀虫、抗糖尿病、降血压、消炎等方面的研究与应用,并展望了其未来可能的发展趋势.

关键词：超分子唑抗癌抗细菌抗真菌抗糖尿病降血压消炎

Novel efficient Synthesis of Chloroethyl Bis-carbazole and Antimicrobial Activities of Its Azole Derivatives

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Novel efficient Synthesis of Chloroethyl Bis-carbazole and A...

Synthesis of Novel Piperazine-propan-2-ol Containing 1,2,4-Triazole

有机合成创新—产业化的新动力——中国化学会全国第三届有机合成化学与过程学术讨论会

作者： Yan,Jianping zhou,chenghe~* (School of Chemistry and Chemical Engineering,Southwest University,400715 Chongqing)

A novel efficient synthesis for chloroethyl bis-carbazole was developed from commercially available carbazole and its azole derivatives were prepared *** the newly synthesized compounds were characterized by H NMR,MS and IR *** antimicrobial activities for some bis-carbazole derivatives were ***-derived bis-carbazole showed good antibacterial activities against *** with MIC value of 8μg/mL.

关键词： bis-carbazole azole synthesis antimicrobial

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Synthesis of Novel Piperazine-propan-2-ol Containing 1,2,4-T...