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.Full text not available from this repository.
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.
|Research Institute, Centre or Group:||Biomolecular Sciences Research Centre|
|Depositing User:||Rebecca Jones|
|Date Deposited:||02 Mar 2012 12:02|
|Last Modified:||02 Mar 2012 12:02|
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