Discovery of potent dipeptidyl peptidase IV inhibitors derived from β-aminoamides bearing substituted [1, 2, 3]-triazolopiperidines for the treatment of type 2 diabetes

Z Shan, M Peng, H Fan, Q Lu, P Lu, C Zhao…

Index: Shan, Zhenwei; Peng, Min; Fan, Houxing; Lu, Qingtao; Lu, Peng; Zhao, Chuansheng; Chen, Yilang Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 6 p. 1731 - 1735

Full Text: HTML

Citation Number: 18

Abstract

A series of novel [1, 2, 3]-triazolopiperidine derivatives 5a–5y were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes, most of the compounds exhibited excellent in vitro potency (IC50< 50nM) against DPP-4. Among these, compound 5d with potent in vitro activity against DPP-4 and good pharmacokinetic profiles exhibited pronounced in vivo efficacy in an oral glucose ...