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