期刊
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS
卷 35, 期 2, 页码 186-190出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijantimicag.2009.07.018
关键词
5-(4-Methylpiperazin-1-yl)-2-[2 '-(3,4-dimethoxyphenyl)-5 '-benzimidazolyl]benzimidazole
资金
- Swedish International Development Agency and Department of Biotechnology
- Department of Science and Technology and Council of Scientific and Industrial Research (New Delhi, India)
New antimicrobials are needed to combat drug resistance and have often been equated with the identification and exploitation of novel targets. This study focused on the synthesis of new benzimidazole analogues with improved DNA minor groove-binding affinity and having lower cytotoxicity to mammalian cells as well as selective targeting of bacterial DNA over host DNA. 5-(4-Methylpiperazin-1-yl)-2-[2'-(3,4-dimethoxyphenyl)-5'-benzimidazolyl]benzimidazole (DMA) cleared bacterial infections from mammalian cell culture without apparent cytotoxicity to mammalian cells. Moreover, DMA inhibited microbial topoisomerase over mammalian topoisomerase, with a 50% inhibitory concentration (IC50) value for human topoisomerase I of >54 mu M compared with an IC50 of <10 mu M for Escherichia coli topoisomerase I in vitro. (C) 2009 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved.
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