Title of article
Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
Author/Authors
Wallace T. Ashton، نويسنده , , Rosemary M. Sisco، نويسنده , , Yu-Hong Dong، نويسنده , , Kathryn A. Lyons، نويسنده , , Huaibing He، نويسنده , , George A. Doss، نويسنده , , Barbara Leiting، نويسنده , , Reshma A. Patel، نويسنده , , Joseph K. Wu، نويسنده , , Frank Marsilio، نويسنده , , Nancy A. Thornberry، نويسنده , , Ann E. Weber، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
2253
To page
2258
Abstract
A series of β-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.
Keywords
Dipeptidyl peptidase IV inhibitors , Diabetes
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795568
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