Discovery and structure-activity relationships of piperidinone-and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV …

…, SJ Ballaron, DWA Beno, AJ Kempf-Grote…

Index: Pei, Zhonghua; Li, Xiaofeng; Von Geldern, Thomas W.; Longenecker, Kenton; Pireh, Daisy; Stewart, Kent D.; Backes, Bradley J.; Lai, Chunqiu; Lubben, Thomas H.; Ballaron, Stephen J.; Beno, David W. A.; Kempf-Grote, Anita J.; Sham, Hing L.; Trevillyan, James M. Journal of Medicinal Chemistry, 2007 , vol. 50, # 8 p. 1983 - 1987

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Citation Number: 66

Abstract

Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the levels of active glucagon-like peptide-1 and glucose-dependent insulinotropic peptide, which are two important incretins for glucose homeostasis. Starting from a high-throughput screening hit, we were able to identify a series of piperidinone-and piperidine-constrained ...