Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity

Authors:	Dhar T G Murali Shen Zhongqi Guo Junqing Liu Chunjian Watterson Scott H Gu Henry H Pitts William J Fleener Catherine A Rouleau Katherine A Sherbina N Z McIntyre Kim W Shuster David J Witmer Mark R Tredup Jeffrey A Chen Bang-Chi Zhao Rulin Bednarz Mark S Cheney Daniel L MacMaster John F Miller Laura M Berry Karen K Harper Timothy W Barrish Joel C Hollenbaugh Diane L Iwanowicz Edwin J

Abstract:	Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme that is involved in the de novo synthesis of purine nucleotides. Novel 2-aminooxazoles were synthesized and tested for inhibition of IMPDH catalytic activity. Multiple analogues based on this chemotype were found to inhibit IMPDH with low nanomolar potency. One of the analogues (compound 23) showed excellent in vivo activity in the inhibition of antibody production in mice and in the adjuvant induced arthritis model in rats.

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