Bioorganic and Medicinal Chemistry Letters p. 1345 - 1348 (2003)
Update date:2022-08-04
Topics:
Chen, Ping
Norris, Derek
Haslow, Kristin D.
Dhar, T. G. Murali
Pitts, William J.
Watterson, Scott H.
Cheney, Daniel L.
Bassolino, Donna A.
Fleener, Catherine A.
Rouleau, Katherine A.
Hollenbaugh, Diane L.
Townsend, Robert M.
Barrish, Joel C.
Iwanowicz, Edwin J.
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.
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