| Literature DB >> 16759869 |
Francis Arhin1, Odette Bélanger, Stéphane Ciblat, Mohammed Dehbi, Daniel Delorme, Evelyne Dietrich, Dilip Dixit, Yanick Lafontaine, Dario Lehoux, Jing Liu, Geoffrey A McKay, Greg Moeck, Ranga Reddy, Yannick Rose, Ramakrishnan Srikumar, Kelly S E Tanaka, Daniel M Williams, Philippe Gros, Jerry Pelletier, Thomas R Parr, Adel Rafai Far.
Abstract
The RNA polymerase holoenzyme is a proven target for antibacterial agents. A high-throughput screening program based on this enzyme from Staphylococcus aureus had previously identified a 2-ureidothiophene-3-carboxylate as a low micromolar inhibitor. An investigation of the relationships between the structures of this class of compounds and their inhibitory- and antibacterial activities is described here, leading to a set of potent RNA polymerase inhibitors with antibacterial activity. Characterization of this bioactivity, including studies of the mechanism of action, is provided, highlighting the power of the reverse chemical genetics approach in providing tools to inhibit the bacterial RNA polymerase.Entities:
Mesh：
Substances：
Year: 2006 PMID： 16759869 DOI： 10.1016/j.bmc.2006.05.035
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641