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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

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Discovery of natural berberine-derived nitroimidazoles as potentially multi-targeting agents against drug-resistant Escherichia coli

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Science China Chemistry 2018年第5期61卷 557-568页

作者： Guo-Biao Zhang Swetha Kameswari Maddili Vijai Kumar Reddy Tangadanchu lavanya gopala Wei-Wei Gao Gui-Xin Cai Cheng-He Zhou Institute of Bioorganic & Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing Municipality School of Chemistry and Chemical Engineering Southwest University

A series of natural berberine-derived nitroimidazoles as novel antibacterial agents were designed, synthesized and characterized by nuclear magnetic resonance(NMR), infrared spectra(IR), and high resolution mass spectra(HRMS) spectra. The antimicrobial evaluation showed that some target molecules exhibited moderate to good inhibitory activities against the tested bacteria and fungi including clinical drug-resistant strains isolated from infected patients. Especially, 2-fluorobenzyl derivative8 f not only gave strong activity against drug-resistant E. coli with the minimal inhibitory concentration(MIC) value of0.003 m M, 33-fold more active than norfloxacin, but also exhibited low toxicity toward RAW 264.7 cells and less propensity to trigger resistance. The aqueous solubility and Clog P values of target compounds were investigated to elucidate the structureactivity relationships. Molecular docking and quantum chemical studies for compound 8 f rationally explained its antibacterial effect. The further exploration of antibacterial mechanism revealed that the highly active compound 8 f could effectively permeabilize E. coli cell membrane and intercalate into DNA isolated from resistant E. coli to form 8 f-DNA complex that might block DNA replication to exert the powerful bioactivities. Compound 8 f could also selectively address resistant E. coli from a mixture of various strains.

关键词： berberine nitroimidazole Escherichia coli DNA membrane permeabilization

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Novel potentially antibacterial naphthalimide-derived metronidazoles:Design,synthesis,biological evaluation and supramolecular interactions with DNA,human serum albumin and topoisomeraseⅡ

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Chinese Chemical Letters 2017年第7期28卷 1369-1374页

作者： Jie Kang Vijai Kumar Reddy Tangadanchu lavanya gopala Wei-Wei Gao Yu Cheng Han-Bo Liu Rong-Xia Geng Shuo Li Cheng-He Zhou Institute of Bioorganic&Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing 400715China School of Chemical Engineering Chongqing University of TechnologyChongqing 400054China Postdoctoral researcher from CSIR-Indian Institute of Chemical Technology Hyderabad 500007India Postdoctoral researcher Sri Venkateswara University Tirupati 517502India

A series of novel naphthalimide-derived metronidazoles as new type of antimicrobial agents were for the first time designed, synthesized and characterized by NMR, IR and HRMS spectra. Experimental results revealed that most of them displayed moderate to good antibacterial activity towards Gram-positive and negative bacteria. Especially, compound 7b was able to not only exhibit effective inhibition towards the growth of P. vulgaris（MIC = 0.002 mmol/m L） and S. dysenteriae（MIC = 0.01 mmol/m L）, but also have rapidly killing effect and prevent the development of bacterial resistance. Further research revealed that the highly active molecule 7b could not only intercalate into calf thymus DNA to form a steady supramolecular complex and thus might block DNA replication to exert the powerful bioactivities, but also be effectively transported by human serum albumin（HSA） via the formation of the 1：1supramolecular complex, in which hydrogen bonds and hydrophobic effect played important roles in the association of compound 7b with HSA. Molecular docking indicated that the supramolecular interactions between 7b and topoisomerase II were driven by hydrogen bonds.

关键词： Metronidazole Naphthalimide Antibacterial Supramolecular DNA

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喹唑酮咪唑类化合物的设计、合成及其抗菌活性与靶向DNA研究

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中国科学：化学 2017年第7期47卷 844-858页

作者：曹泉诚王辉 Tangadanchu Vijai Kumar Reddy gopala lavanya 蔡桂鑫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

多药耐药菌的频繁出现已日益严重威胁人类健康,开发结构新型的抗菌药物已成为全世界战胜耐药菌的重要课题.本文设计合成了一系列具有抗微生物潜力的酰腙桥链的喹唑酮咪唑类新化合物,其结构经核磁共振氢谱(~1H NMR)、核磁共振碳谱(^(13)C... 详细信息

多药耐药菌的频繁出现已日益严重威胁人类健康,开发结构新型的抗菌药物已成为全世界战胜耐药菌的重要课题.本文设计合成了一系列具有抗微生物潜力的酰腙桥链的喹唑酮咪唑类新化合物,其结构经核磁共振氢谱(~1H NMR)、核磁共振碳谱(^(13)C NMR)和高分辨质谱(HRMS)进行表征.生物活性研究发现,一些目标化合物具有较好的抗微生物活性,特别是十八烷基衍生物6h和4-氟苄基取代的化合物7i,抗痢疾杆菌和大肠杆菌DH52的活性是氯霉素的2.5~3.3倍,抗黄曲霉菌活性是临床药物氟康唑的28和8.4倍.用紫外-可见光谱法进行了高活性化合物7i靶向DNA的初步研究,发现咪唑衍生物7i可嵌入小牛胸腺DNA形成7i-DNA超分子络合物,从而阻断DNA复制,展现出较好的抗细菌活性.分子模拟研究表明,活性分子7i与DNA碱基通过氢键结合.该类化合物作为新型抗真菌黄曲霉菌专一特效药及新型抗细菌药值得深入研究.

关键词：喹唑酮抗细菌抗真菌咪唑酰腙分子对接 DNA

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