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Novel potentially antibacterial naphthalimide-derived metronidazoles: Design, synthesis, biological evaluation and supramolecular interactions with DNA, human serum albumin and topoisomerase Ⅱ
  • ISSN号:1001-8417
  • 期刊名称:《中国化学快报:英文版》
  • 时间:0
  • 分类:S859.796[农业科学—临床兽医学;农业科学—兽医学;农业科学—畜牧兽医] TQ463.53[化学工程—制药化工]
  • 作者机构:[1]Institute of Bioorganic & Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China, [2]School of Chemistry and Chemical Engineering, Qiannan Normal University for Nationalities, Duyun, Guizhou 558000, China
  • 相关基金:This work was partially supported by the National Natural Science Foundation of China [(Nos. 21372186, 21672173), the Research Fund for International Young Scientists from International (Regional) Cooperation and Exchange Program (No. 81650110529)] and Chongqing Special Foundation for Postdoctoral Research Proposal (Xm2015031 ).
中文摘要:

当新潜在的抗菌剂代理人被 1 H NMR, 13 C NMR,红外和 HRMS 系列。抗菌剂试金表明了目标混合物给了的那一些对好抗菌剂和抗真菌的活动中等。N-1 导出 benzotriazole 5e, N-2 导出对测试的一些的展出珍贵禁止的功效拉紧的 benzotriazole 6a。特别,衍生物 6a 对 C 给了优异抗真菌的功效。utilis, S。cerevisiae 和 A。flavus (MIC=0.01, 0.02, 0.02biguity,和在感情方面、支持的亲戚关系关系中产生的紧张的焦点,还也开发资源。主要争论是有 precarity ,和那种亲戚关系的不同模式,哪个主要在一个不明确的世界上被认为是安全,吗能事实上加重动荡的 condition.Lentrepreneuriat pr 賦?觧???铧????釦?觧???藦??藦????賧??????闧?闦?蓦?觧????  吗??

英文摘要:

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.

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期刊信息
  • 《中国化学快报:英文版》
  • 中国科技核心期刊
  • 主管单位:中国科学技术协会
  • 主办单位:中国化学会
  • 主编:
  • 地址:北京市先农坛街1号
  • 邮编:100050
  • 邮箱:cclbj@imm.ac.cn
  • 电话:010-63165638
  • 国际标准刊号:ISSN:1001-8417
  • 国内统一刊号:ISSN:11-2710/O6
  • 邮发代号:2-915
  • 获奖情况:
  • 1998、1999年获中国科协和国家自然科学基金,高科技学术期刊资助二等奖,2000年获国家自然基金委重点期刊一等奖
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  • 被引量:760