Abstract
A series of substituted imidazopiperidine amides has been prepared and evaluated for inhibition of dipeptidyl peptidase IV (DPP-4). Substitution at the 1- and 3-positions produced increased selectivity for DPP-4 relative to DPP-8 and DPP-9. Compounds in this series had IC(50) values as low as 5.8 nM for inhibition of DPP-4.
MeSH terms
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Amides / chemistry
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Diabetes Mellitus / drug therapy*
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Dipeptidyl-Peptidase IV Inhibitors*
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Humans
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Hypoglycemic Agents / pharmacology*
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Hypoglycemic Agents / therapeutic use
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Piperidines / chemistry
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Piperidines / pharmacology*
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Piperidines / therapeutic use
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology*
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Protease Inhibitors / therapeutic use
Substances
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Amides
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Dipeptidyl-Peptidase IV Inhibitors
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Hypoglycemic Agents
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Piperidines
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Protease Inhibitors