3,4-Dimethoxyphenyl bis-benzimidazole, a novel DNA topoisomerase inhibitor that preferentially targets Escherichia coli topoisomerase I
Author(s) -
Sandhya Bansal,
D. K. Sinha,
Manish Kumar Singh,
Bokun Cheng,
Yuk-Ching Tse-Dinh,
Vibha Tandon
Publication year - 2012
Publication title -
journal of antimicrobial chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.124
H-Index - 194
eISSN - 1460-2091
pISSN - 0305-7453
DOI - 10.1093/jac/dks322
Subject(s) - topoisomerase , dna gyrase , topoisomerase iv , escherichia coli , ethidium bromide , dna supercoil , biology , topoisomerase inhibitor , benzimidazole , microbiology and biotechnology , dna , biochemistry , chemistry , dna replication , organic chemistry , gene
Antibiotic resistance in bacterial pathogens is a serious clinical problem. Novel targets are needed to combat increasing drug resistance in Escherichia coli. Our objective is to demonstrate that 2-(3,4-dimethoxyphenyl)-5-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2yl]-1H-benzimidazole (DMA) inhibits E. coli DNA topoisomerase I more strongly than human topoisomerase I. In addition, DMA is non-toxic to mammalian cells at antibiotic dosage level.
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