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Old class but new dimethoxy analogue of benzimidazole: a bacterial topoisomerase I inhibitor

Authors
Journal
International Journal of Antimicrobial Agents
0924-8579
Publisher
Elsevier
Publication Date
Volume
35
Issue
2
Identifiers
DOI: 10.1016/j.ijantimicag.2009.07.018
Keywords
  • 5-(4-Methylpiperazin-1-Yl)-2-[2′-(3
  • 4-Dimethoxyphenyl)-5′-Benzimidazolyl]Benzimidazole

Abstract

Abstract 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 (IC 50) value for human topoisomerase I of >54 μM compared with an IC 50 of <10 μM for Escherichia coli topoisomerase I in vitro.

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