| Title : Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors - Corbett_2007_Bioorg.Med.Chem.Lett_17_6707 |
| Author(s) : Corbett JW , Dirico K , Song W , Boscoe BP , Doran SD , Boyer D , Qiu X , Ammirati M , VanVolkenburg MA , McPherson RK , Parker JC , Cox ED |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :6707 , 2007 |
|
Abstract :
The cis-3-amino-4-(2-cyanopyrrolidide)-pyrrolidine template has been shown to afford low nanomolar inhibitors of human DPP-IV that exhibit a robust PK/PD profile. An X-ray co-crystal structure of 5 confirmed the proposed mode of binding. The potent single digit DPP-IV inhibitor 53 exhibited a preferred PK/PD profile in preclinical animal models and was selected for additional profiling. |
| PubMedSearch : Corbett_2007_Bioorg.Med.Chem.Lett_17_6707 |
| PubMedID: 17977724 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl-34Q |
| Gene_locus | human-DPP4 |
| Structure | 2RIP |
Corbett JW, Dirico K, Song W, Boscoe BP, Doran SD, Boyer D, Qiu X, Ammirati M, VanVolkenburg MA, McPherson RK, Parker JC, Cox ED (2007)
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors
Bioorganic & Medicinal Chemistry Lett
17 :6707
Corbett JW, Dirico K, Song W, Boscoe BP, Doran SD, Boyer D, Qiu X, Ammirati M, VanVolkenburg MA, McPherson RK, Parker JC, Cox ED (2007)
Bioorganic & Medicinal Chemistry Lett
17 :6707