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Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors

Identification of novel and potent isoquinoline aminooxazole-Based IMPDH inhibitors

Authors :
Edwin J. Iwanowicz
Kristin D. Haslow
Donna A. Bassolino
Derek J. Norris
Robert M. Townsend
Daniel L. Cheney
Joel C. Barrish
William J. Pitts
Scott H. Watterson
Katherine A. Rouleau
Catherine A. Fleener
T. G. Murali Dhar
Diane Hollenbaugh
Ping Chen
Source :
Bioorganic & Medicinal Chemistry Letters. 13:1345-1348
Publication Year :
2003
Publisher :
Elsevier BV, 2003.

Abstract

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.

Details

ISSN :
0960894X
Volume :
13
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....53fc56fb4aaf95da3433bd20e11fd0d9
Full Text :
https://doi.org/10.1016/s0960-894x(03)00107-0