Literature DB >> 20660693

Furanyl-rhodanines are unattractive drug candidates for development as inhibitors of bacterial RNA polymerase.

Katherine R Mariner1, Rachel Trowbridge, Anil K Agarwal, Keith Miller, Alex J O'Neill, Colin W G Fishwick, Ian Chopra.   

Abstract

Previous studies suggest that furanyl-rhodanines might specifically inhibit bacterial RNA polymerase (RNAP). We further explored three compounds from this class. Although they inhibited RNAP, each compound also inhibited malate dehydrogenase and chymotrypsin. Using biosensors responsive to inhibition of macromolecular synthesis and membrane damaging assays, we concluded that in bacteria, one compound inhibited DNA synthesis and another caused membrane damage. The third rhodanine lacked antibacterial activity. We consider furanyl-rhodanines to be unattractive RNAP inhibitor drug candidates.

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Year:  2010        PMID: 20660693      PMCID: PMC2944609          DOI: 10.1128/AAC.00753-10

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  15 in total

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