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ID: ALA1136691

Journal: Bioorg Med Chem Lett

Title: Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors.

Authors: Chen P, Norris D, Haslow KD, Murali Dhar TG, Pitts WJ, Watterson SH, Cheney DL, Bassolino DA, Fleener CA, Rouleau KA, Hollenbaugh DL, Townsend RM, Barrish JC, Iwanowicz EJ.

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.

CiteXplore: 12657279

DOI: 10.1016/s0960-894x(03)00107-0