期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 111, 期 -, 页码 160-182出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.01.052
关键词
Quinolone; Benzimidazole; Anti-MRSA; DNA; Topoisomerase
资金
- National Natural Science Foundation of China [21172181, 21372186]
- National Natural Science Foundation of China [Research Fund for International Young Scientists from International (Regional) Cooperation and Exchange Program NSFC] [81450110451]
- Specialized Research Fund for the Doctoral Program of Higher Education of China [SRFDP 20110182110007]
A series of novel benzimidazole quinolones as potential antimicrobial agents were designed and synthesized. Most of the prepared compounds exhibited good or even stronger antimicrobial activities in comparison with reference drugs. The most potent compound 15m was membrane active and did not trigger the development of resistance in bacteria. It not only inhibited the formation of biofilms but also disrupted the established Staphylococcus aureus and Escherichia coli biofilms. It was able to inhibit the relaxation activity of E. coli topoisomerase IV at 10 mu M concentration. Moreover, this compound also showed low toxicity against mammalian cells. Molecular modeling and experimental investigation of compound 15m with DNA suggested that this compound could effectively bind with DNA to form a steady 15m-DNA complex which might further block DNA replication to exert the powerful bioactivities. (C) 2016 Elsevier Masson SAS. All rights reserved.
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