Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors

被引：30

作者：

Chen, P

Norris, D

Haslow, KD

Dhar, TGM

Pitts, WJ

Watterson, SH

Cheney, DL

Bassolino, DA

Fleener, CA

Rouleau, KA

Hollenbaugh, DL

Townsend, RM

Barrish, JC

Iwanowicz, EJ

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Discovery Chem, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Immunol Inflammat & Pulm Drug Discovery, Princeton, NJ 08543 USA

[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Comp Aided Drug Design, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(03)00107-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Screening of our in-house compound collection led to the discovery of 5-bromo-6-amino-2-isoquinoline I as a weak inhibitor of IMPDH. Subsequent optimization of 1 afforded a series of novel 2-isoquinolinoaminooxazole-based inhibitors, represented by 17, with single-digit nanomolar potency against the enzyme. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1345 / 1348

页数：4

共 19 条

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