| 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_2007_Bioorg.Med.Chem.Lett_17_5638 |
| 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 |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :5638 , 2007 |
|
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. |
| PubMedSearch : Wright_2007_Bioorg.Med.Chem.Lett_17_5638 |
| PubMedID: 17822893 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | 3-amino-4-phenyl-pyrrolidine-15B |
| Gene_locus | human-DPP4 |
| Structure | 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 (2007)
(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
Bioorganic & Medicinal Chemistry Lett
17 :5638
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 (2007)
Bioorganic & Medicinal Chemistry Lett
17 :5638