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

MARINER, K R, TROWBRIDGE, R, AGARWAL, A K, MILLER, Keith, O'NEILL, A J, FISHWICK, C W and CHOPRA, I (2010). Furanyl-rhodanines are unattractive drug candidates for development as inhibitors of bacterial RNA polymerase. Antimicrobial Agents and Chemotherapy, 54 (10), 4506-4509.

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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.

Item Type:	Article
Research Institute, Centre or Group - Does NOT include content added after October 2018:	Biomedical Research Centre
Identification Number:	https://doi.org/10.1128/AAC.00753-10
Page Range:	4506-4509
Depositing User:	Rebecca Jones
Date Deposited:	02 Mar 2012 12:02
Last Modified:	18 Mar 2021 10:15
URI:	https://shura.shu.ac.uk/id/eprint/4509

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