Abstract
A new series of cyano-pyrazoline derivatives with secondary amine at P-2 site was synthesized through achiral and chiral synthetic methods and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 5i revealed good in vivo efficacy (ED50: 4.1 mg/kg; in vivo DP-IV inhibition). Also chiral derivative (11b) having (S)-configuration of compound 5i was found to be more potent.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Caco-2 Cells
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Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / antagonists & inhibitors*
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Dipeptidyl-Peptidases and Tripeptidyl-Peptidases / metabolism
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Humans
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / pharmacology
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Mice
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Mice, Inbred C57BL
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / pharmacology
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Pyrazoles / chemical synthesis*
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Pyrazoles / pharmacology
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Rats
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Swine
Substances
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Hypoglycemic Agents
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Protease Inhibitors
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Pyrazoles
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DP IV-related protease, human
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Dipeptidyl-Peptidases and Tripeptidyl-Peptidases