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2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV |
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| Authors: | Haffner Curt D McDougald Darryl L Reister Steven M Thompson Brian D Conlee Christopher Fang Jing Bass Jonathan Lenhard James M Croom Dallas Secosky-Chang Melissa B Tomaszek Thaddeus McConn Donavon Wells-Knecht Kevin Johnson Paul R |
| Affiliation: | Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA. curt.d.haffner@gsk.com |
| Abstract: | 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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