Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced p K a: antibacterial agents with an improved safety profile

…, J Comita-Prevoir, M Cronin, DE Ehmann…

文献索引：Reck, Folkert; Alm, Richard A.; Brassil, Patrick; Newman, Joseph V.; Ciaccio, Paul; McNulty, John; Barthlow, Herbert; Goteti, Kosalaram; Breen, John; Comita-Prevoir, Janelle; Cronin, Mark; Ehmann, David E.; Geng, Bolin; Godfrey, Andrew Aydon; Fisher, Stewart L. Journal of Medicinal Chemistry, 2012 , vol. 55, # 15 p. 6916 - 6933

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被引用次数: 43

摘要

Novel non-fluoroquinolone inhibitors of bacterial type II topoisomerases (DNA gyrase and topoisomerase IV) are of interest for the development of new antibacterial agents that are not impacted by target-mediated cross-resistance with fluoroquinolones. N-Linked amino piperidines, such as 7a, generally show potent antibacterial activity, including against quinolone-resistant isolates, but suffer from hERG inhibition (IC50= 44 μM for 7a) and QT ...