| Literature DB >> 12361393 |
Tasir S Haque1, Seifu Tadesse, Jovita Marcinkeviciene, M John Rogers, Christine Sizemore, Lisa M Kopcho, Karen Amsler, Lisa D Ecret, Dong Liang Zhan, Frank Hobbs, Andrew Slee, George L Trainor, Andrew M Stern, Robert A Copeland, Andrew P Combs.
Abstract
The identification of several potent pyrazole-based inhibitors of bacterial dihydroorotate dehydrogenase (DHODase) via a directed parallel synthetic approach is described below. The initial pyrazole-containing lead compounds were optimized for potency against Helicobacter pylori DHODase. Using three successive focused libraries, inhibitors were rapidly identified with the following characteristics: K(i) < 10 nM against H. pylori DHODase, sub-microg/mL H. pylori minimum inhibitory concentration activity, low molecular weight, and >10 000-fold selectivity over human DHODase.Entities:
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Year: 2002 PMID： 12361393 DOI： 10.1021/jm020112w
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446