| Title : Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors - Edmondson_2008_Bioorg.Med.Chem.Lett_18_2409 |
| Author(s) : Edmondson SD , Wei L , Xu J , Shang J , Xu S , Pang J , Chaudhary A , Dean DC , He H , Leiting B , Lyons KA , Patel RA , Patel SB , Scapin G , Wu JK , Beconi MG , Thornberry NA , Weber AE |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :2409 , 2008 |
|
Abstract :
The synthesis, selectivity, rat pharmacokinetic profile, and drug metabolism profiles of a series of potent fluoroolefin-derived DPP-4 inhibitors (4) are reported. A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors. |
| PubMedSearch : Edmondson_2008_Bioorg.Med.Chem.Lett_18_2409 |
| PubMedID: 18331795 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | Flouroolefin-1 Flouroolefin-2 |
| Gene_locus | human-DPP4 |
| Structure | 3C43 3C45 |
Edmondson SD, Wei L, Xu J, Shang J, Xu S, Pang J, Chaudhary A, Dean DC, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Scapin G, Wu JK, Beconi MG, Thornberry NA, Weber AE (2008)
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett
18 :2409
Edmondson SD, Wei L, Xu J, Shang J, Xu S, Pang J, Chaudhary A, Dean DC, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Scapin G, Wu JK, Beconi MG, Thornberry NA, Weber AE (2008)
Bioorganic & Medicinal Chemistry Lett
18 :2409