Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
| Autor: | Reshma A. Patel, Hong Dong, Ann E. Weber, Joseph K. Wu, Wallace T. Ashton, George A. Doss, Huaibing He, Nancy A. Thornberry, Barbara Leiting, Kathryn A. Lyons, Frank Marsilio, Rosemary Sisco |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
Stereochemistry
medicine.drug_class Dipeptidyl Peptidase 4 Clinical Biochemistry Pharmaceutical Science Carboxamide Pyrazole Biochemistry Chemical synthesis chemistry.chemical_compound Piperidines Drug Discovery medicine Protease Inhibitors Isoxazole Thiazole Oxazoles Molecular Biology Oxazole Bicyclic molecule biology Organic Chemistry Isoxazoles Thiazoles chemistry Enzyme inhibitor biology.protein Pyrazoles Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 15:2253-2258 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2005.03.012 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect