Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors |
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| Authors: | Chen Ping Caldwell Charles G Ashton Wallace Wu Joseph K He Huaibing Lyons Kathryn A Thornberry Nancy A Weber Ann E |
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| Institution: | a Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
b Department of Metabolic Disorders-Diabetes, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA |
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| Abstract: | A series of 4-amino cyclohexanes and 4-substituted piperidines were prepared and evaluated for inhibition of DPP-4. Analog 20q displayed both good DPP-4 potency and selectivity against other proteases, while derivative 20k displayed long half life and modest oral bioavailability in rat. The most potent analog, 3-(5-aminocarbonylpyridyl piperidine 53j, displayed excellent DPP-4 activity with good selectivity versus other proline enzymes. |
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