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ID: ALA1145410

Journal: Bioorg Med Chem Lett

Title: Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.

Authors: Cox JM, Harper B, Mastracchio A, Leiting B, Sinha Roy R, Patel RA, Wu JK, Lyons KA, He H, Xu S, Zhu B, Thornberry NA, Weber AE, Edmondson SD.

Abstract: Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassium channel, calcium channel, Cyp2D6, and pharmacokinetic profiles.

CiteXplore: 17562364

DOI: 10.1016/j.bmcl.2007.05.087