2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV

Curt D. Haffner,Darryl L. McDougald,Steven M. Reister,Brian D. Thompson,Christopher Conlee,Jing Fang,Jonathan Bass,James M. Lenhard,Dallas Croom,Melissa B. Secosky-Chang,Thaddeus Tomaszek,Donavon McConn,Kevin Wells-Knecht,Paul R. Johnson

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

We report the synthesis and biological activity of a series of 2-cyano-4-fluoro-1-thiovalylpyrrolidine inhibitors of DPP-IV. Within this series, compound 19 provided a potent, selective, and orally active DPP-IV inhibitor which demonstrated a very long duration of action in both rat and dog.

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关键词

DPP-IV,Glucagon-like peptide 1,Glucose-dependent inhibitory polypeptide,Dipeptidyl peptidase IV

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