1026798-82-2Relevant academic research and scientific papers
Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase
Haque, Tasir S.,Tadesse, Seifu,Marcinkeviciene, Jovita,Rogers, M. John,Sizemore, Christine,Kopcho, Lisa M.,Amsler, Karen,Ecret, Lisa D.,Zhan, Dong Liang,Hobbs, Frank,Slee, Andrew,Trainor, George L.,Stern, Andrew M.,Copeland, Robert A.,Combs, Andrew P.
, p. 4669 - 4678 (2007/10/03)
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: Ki 10 000-fold selectivity over human DHODase.
