(3R, 4S)-4-(2, 4, 5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: Synthesis, in vitro, in vivo, and X-ray crystallographic characterization

…, JS Lillquist, S Liu, LD McClure, RK McPherson…

Index: Wright, Stephen W.; Ammirati, Mark J.; Andrews, Kim M.; Brodeur, Anne M.; Danley, Dennis E.; Doran, Shawn D.; Lillquist, Jay S.; Liu, Shenping; McClure, Lester D.; McPherson, R. Kirk; Olson, Thanh V.; Orena, Stephen J.; Parker, Janice C.; Rocke, Benjamin N.; Soeller, Walter C.; Soglia, Carolyn B.; Treadway, Judith L.; VanVolkenburg, Maria A.; Zhao, Zhengrong; Cox, Eric D. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 20 p. 5638 - 5642

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Citation Number: 11

Abstract

A series of pyrrolidine based inhibitors of dipeptidyl peptidase IV were developed from a high throughput screening hit for the treatment of type 2 diabetes. Potency, selectivity, and pharmacokinetic properties were optimized resulting in the identification of a pre-clinical candidate for further profiling.