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

作者信息

Cox Jason M, Harper Bart, Mastracchio Anthony, Leiting Barbara, Sinha Roy Ranabir, Patel Reshma A, Wu Joseph K, Lyons Kathryn A, He Huaibing, Xu Shiyao, Zhu Bing, Thornberry Nancy A, Weber Ann E, Edmondson Scott D

机构信息

Merck Research Laboratories, Department of Medicinal Chemistry, PO Box 2000, Rahway, NJ 07065, USA.

出版信息

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4579-83. doi: 10.1016/j.bmcl.2007.05.087. Epub 2007 Jun 2.

DOI:10.1016/j.bmcl.2007.05.087

PMID:17562364

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.

摘要

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