A new class of small molecule RNA polymerase inhibitors with activity against rifampicin-resistant Staphylococcus aureus

…, D Lehoux, J Liu, GA McKay, G Moeck, R Reddy…

文献索引：Arhin, Francis; Belanger, Odette; Ciblat, Stephane; Dehbi, Mohammed; Delorme, Daniel; Dietrich, Evelyne; Dixit, Dilip; Lafontaine, Yanick; Lehoux, Dario; Liu, Jing; McKay, Geoffrey A.; Moeck, Greg; Reddy, Ranga; Rose, Yannick; Srikumar, Ramakrishnan; Tanaka, Kelly S.E.; Williams, Daniel M.; Gros, Philippe; Pelletier, Jerry; Parr Jr., Thomas R.; Far, Adel Rafai Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 17 p. 5812 - 5832

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被引用次数: 39

摘要

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 ...