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.
Published by Elsevier Ltd.
MeSH terms
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Animals
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Biological Availability
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Cyclohexanes / chemical synthesis*
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Cyclohexanes / pharmacokinetics
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Cyclohexanes / pharmacology*
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Dipeptidyl-Peptidase IV Inhibitors / chemical synthesis*
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Dipeptidyl-Peptidase IV Inhibitors / pharmacokinetics
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Dipeptidyl-Peptidase IV Inhibitors / pharmacology*
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Half-Life
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Piperidines / chemical synthesis*
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Piperidines / pharmacokinetics
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Piperidines / pharmacology*
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Rats
Substances
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Cyclohexanes
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Dipeptidyl-Peptidase IV Inhibitors
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Piperidines