Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors

详细信息    查看全文

• 作者：Chen ; Ping ; Norris ; Derek ; Haslow ; Kristin D. ; Murali Dhar ; T. G. ; Pitts ; William J. ; Watterson ; Scott H. ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2003
• 出版时间：April 7, 2003
• 年：2003
• 卷：13
• 期：7
• 页码：1345-1348
• 全文大小：168 K

文摘

Screening of our in-house compound collection led to the discovery of 5-bromo-6-amino-2-isoquinoline 1 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.