| Title : Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole - Ashton_2005_Bioorg.Med.Chem.Lett_15_2253 |
| Author(s) : Ashton WT , Sisco RM , Dong H , Lyons KA , He H , Doss GA , Leiting B , Patel RA , Wu JK , Marsilio F , Thornberry NA , Weber AE |
| Ref : Bioorganic & Medicinal Chemistry Lett , 15 :2253 , 2005 |
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Abstract :
A series of beta-aminoacylpiperidines bearing various fused five-membered heterocyclic rings was synthesized as dipeptidyl peptidase IV inhibitors. Potent and relatively selective inhibition could be obtained, depending on choice of heterocycle, regioisomerism, and substitution. In particular, one analog (74, DPP-IV IC50=26 nM) exhibited good oral bioavailability and acceptable half-life in the rat, albeit with rather high clearance. |
| PubMedSearch : Ashton_2005_Bioorg.Med.Chem.Lett_15_2253 |
| PubMedID: 15837304 |
Ashton WT, Sisco RM, Dong H, Lyons KA, He H, Doss GA, Leiting B, Patel RA, Wu JK, Marsilio F, Thornberry NA, Weber AE (2005)
Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
Bioorganic & Medicinal Chemistry Lett
15 :2253
Ashton WT, Sisco RM, Dong H, Lyons KA, He H, Doss GA, Leiting B, Patel RA, Wu JK, Marsilio F, Thornberry NA, Weber AE (2005)
Bioorganic & Medicinal Chemistry Lett
15 :2253