Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors
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.
Kumar, Pramod; Agarwal, Shiv K; Bhakuni, D S, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1992, vol. 31, # 3, p. 177 - 182
Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors
作者:Ping Chen、Derek Norris、Kristin D. Haslow、T.G. Murali Dhar、William J. Pitts、Scott H. Watterson、Daniel L. Cheney、Donna A. Bassolino、Catherine A. Fleener、Katherine A. Rouleau、Diane L. Hollenbaugh、Robert M. Townsend、Joel C. Barrish、Edwin J. Iwanowicz
DOI:10.1016/s0960-894x(03)00107-0
日期:2003.4
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.