Furanyl-rhodanines Are Unattractive Drug Candidates for Development As Inhibitors of Bacterial RNA Polymerase

Overview

Journal Antimicrob Agents Chemother

Publisher American Society for Microbiology

Specialty Pharmacology

Date 2010 Jul 28

PMID 20660693

Citations 8

Authors

Katherine R Mariner

Rachel Trowbridge

Anil K Agarwal

Keith Miller

Alex J ONeill

Colin W G Fishwick

Ian Chopra

Affiliations

Soon will be listed here.

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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