Structure Report for: 2QJR

Wright SW, Ammirati MJ, Andrews KM, Brodeur AM, Danley DE, Doran SD, Lillquist JS, Liu S, McClure LD, McPherson RK, Olson TV, Orena SJ, Parker JC, Rocke BN, Soeller WC, Soglia CB, Treadway JL, Vanvolkenburg MA, Zhao Z, Cox ED

Title: (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
Wright SW, Ammirati MJ, Andrews KM, Brodeur AM, Danley DE, Doran SD, Lillquist JS, Liu S, McClure LD and Cox ED <10 more author(s)> Wright SW, Ammirati MJ, Andrews KM, Brodeur AM, Danley DE, Doran SD, Lillquist JS, Liu S, McClure LD, McPherson RK, Olson TV, Orena SJ, Parker JC, Rocke BN, Soeller WC, Soglia CB, Treadway JL, VanVolkenburg MA, Zhao Z, Cox ED (- 10)
Ref: Bioorganic & Medicinal Chemistry Lett, 17:5638, 2007 : PubMed
Abstract


ESTHER: Wright_2007_Bioorg.Med.Chem.Lett_17_5638
PubMedSearch: Wright 2007 Bioorg.Med.Chem.Lett 17 5638
PubMedID: 17822893
Gene_locus related to this paper: human-DPP4
Inhibitor(s) related to this paper: 3-amino-4-phenyl-pyrrolidine-15B

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.