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中国化学会全国第十二届有机合成化学学术研讨会

作者： maddili,swetha kameswari Zhou,Cheng-He Institute of Bioorganic ＆ Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest University

Imidazobenzothiazole derivatives are very vital class of heterocycles distributed in nature and exhibit diverse biological *** we have developed novel imidazo[2,1-b]benzothiazole triazoles as new type of antimicrobial *** synthesized compounds were confirmed by 1H-NMR and MS spectra and were screened for their antimicrobial activity.

关键词： benzothiazoles triazole fluconoloze synthesis

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Thiazoles-based Supermolecules As Anticancer Agents

Thiazoles-based Supermolecules As Anticancer Agents

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全国第十七届大环化学暨第九届超分子化学学术研讨会

作者：文思奇 maddili swetha kameswari 周成合 School of Chemistry and Chemical Engineering Southwest University

＜正＞Thiazole and its benzothiazole is an important type of aromatic heterocycles with nitrogen and sulfur *** special structure of thiazole ring endows its derivatives to exhibit wide potential applications in chemi... 详细信息

关键词： Thiazole Benzothiazole Supramolecular drug Anticancer

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Coumarin-derived Metronidazoles:Design,Synthesis,Activity and Supramolecular Interaction with DNA

Coumarin-derived Metronidazoles:Design,Synthesis,Activity an...

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全国第十七届大环化学暨第九届超分子化学学术研讨会

作者： Kannekanti Vijaya Kumar maddili swetha kameswari 周成合 School of Chemistry and Chemical Engineering Southwest University Indian Institute of Chemical Technology(IICT)

＜正＞Novel coumarin metronidazoles as antimicrobial agents were synthesized and their synthesized compounds were confirmed by NMR and MS *** new compounds exhibited strong antimicrobial activities against four Gram-p... 详细信息

关键词： Coumarin Metronidazole Antimicrobial

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硝基咪唑杂环药物化学研究进展

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中国科学：化学 2019年第2期49卷 230-255页

作者：李珍珍 maddili swetha kameswari TangadanchuVijai Kumar Reddy Bheemanaboina Rammohan R.Yadav 林健梅杨仁国蔡桂鑫周成合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 电子科技大学临床医学院成都610072

硝基咪唑是一类特殊结构的杂环,五元芳香杂环咪唑与硝基的共缀使其衍生物呈现广泛的应用潜力,在药物、人工诊断剂与人工探针等相关领域研究异常活跃,尤其是在医药方面作为人工合成的化学药物已在临床中广泛用于抗癌、抗菌、抗寄生虫等,... 详细信息

硝基咪唑是一类特殊结构的杂环,五元芳香杂环咪唑与硝基的共缀使其衍生物呈现广泛的应用潜力,在药物、人工诊断剂与人工探针等相关领域研究异常活跃,尤其是在医药方面作为人工合成的化学药物已在临床中广泛用于抗癌、抗菌、抗寄生虫等,备受关注.本文结合本课题组相关研究,参考国内外近期文献,系统地综述了硝基咪唑类化合物在药物化学领域的研究与应用,包括抗肿瘤、抗细菌、抗真菌、抗寄生虫、抗结核、抗高血压以及作为人工诊断剂与病理探针、超分子基体等领域的当前现状,展望了其未来可能的发展趋势.希望该评述能为硝基咪唑类杂环化合物的多用途开发提供有益的指导.

关键词：硝基咪唑抗肿瘤抗感染人工诊断剂与病理探针超分子基体

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Synthesis of Novel Chalcone-based Benzothiazoles as Brugia Malayi Thymidylate Kinase Inhibitors

Synthesis of Novel Chalcone-based Benzothiazoles as Brugia M...

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中国化学会全国第十二届有机合成化学学术研讨会

作者： Avula,Srinivasa Rao Wen,Si-Qi maddili,swetha kameswari Sashidhara,Koneni V. Zhou,Cheng-He Institute of Bioorganic & Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University CSIR-Central Drug Research Institute

A series of novel chalcone-based benzothiazoles as brugia malayi thymidylate kinase inhibitors have been synthesized and evaluated for their Brugia malayi thymidylate kinase（BmT MK） enzyme inhibition *** selectivity towards BmT MK was *** prepared compound 1 was found to show strong interactions with the BmT MK active *** docking study revealed that the interactions was corroborated well with their antifilarial activities in vitro from the experimental *** prepared benzothiazole derivatives are selective towards the BmT MK enzyme and may be served as potential therapeutic agents against filariasis.

关键词： chalcone benzothiazole thymidylate kinase antifilarial activity brugia malayi

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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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New 2-aminothiazolyl quinolones as DNA intercalators

New 2-aminothiazolyl quinolones as DNA intercalators

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全国第十八届大环化学暨第十届超分子化学学术讨论会

作者：程宇 swetha kameswari maddili 周成合 School of Chemistry and Chemical Engineering Southwest University

＜正＞Quinolones are one of the most commonly prescribed antibacterial drugs and have been extensively used to combat with a number of bacterial ***,with the wide use even overuse of these drugs,the resistance to quin... 详细信息

关键词： Quinolone Aminothiazole DNA intercalator

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Synthesis of Mannich Bases of 2-Arylimidazo[2,1-b]benzothiazoles

Synthesis of Mannich Bases of 2-Arylimidazo[2,1-b]benzothiaz...

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中国化学会第九届全国有机化学学术会议

作者： swetha kameswari maddili 文思奇周成合 Institute of Bioorganic & Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing Municipality School of Chemistry and Chemical Engineering Southwest University

A novel class of Mannich bases of imidazobenzothiazole derivatives were designed and synthesized and characterized adequately by IR,H NMR,MS,and C NMR spectroscopy.

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Synthesis of Pyrimidine Azoles as DNA-targeting Antibacterial Agents

Synthesis of Pyrimidine Azoles as DNA-targeting Antibacteria...

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中国化学会·第十五届全国有机合成化学学术研讨会

作者： Di Li swetha kameswari maddili 周成合 School of Chemistry and Chemical Engineering Southwest University 西南大学

A series of pyrimidine-based azoles as novel structural type of potentially DNA-targeting antibacterial agents were designed, synthesized and characterized from *** antibacterial evaluation revealed that some target compounds could selectively and effectively inhibit the growth of Enterococcus faecalis with low MIC value of 8-32 μg/*** docking study discovered that the high active compound could bind with DNA gyrase by hydrogen bonds and other weak *** further exploration disclosed that the active molecule could also effectively intercalate into antibacterial DNA and form a steady supramolecular complex with DNA, which might further block DNA replication to exert the powerful antibacterial effects.

关键词： pyrimidine azole antibacterial DNA drug resistance

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Novel Imidazo[2,1-b]benzothiazole Benzimidazoles: Synthesis,and Supramolecular Interaction with Calf Thymus DNA

Novel Imidazo[2,1-b]benzothiazole Benzimidazoles: Synthesis,...

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全国第十八届大环化学暨第十届超分子化学学术讨论会

作者： swetha kameswari maddili Kannekanti Vijaya Kumar 周成合 School of Chemistry and Chemical Engineering Southwest University

＜正＞A stipulating requirement is increasing for potent antimicrobial agents that can deal with the infectious diseases caused by destructive bacteria and *** studies disclosed that benzimidazoles have substantial ability to restrict the growth of bacterial and fungal ***,we have intended to alter imidazo[2,1-b]benzothiazole moiety by incorporating benzimidazole nucleus which has ended up in a

关键词： imidazo[2,1-b] benzothiazole benzimidazole bacterial fungal

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