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Bioorg Med Chem Lett ; 15(23): 5257-61, 2005 Dec 01.
Article in English | MEDLINE | ID: mdl-16168640

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.


Subject(s)
Dipeptidyl Peptidase 4/metabolism , Protease Inhibitors/chemistry , Protease Inhibitors/pharmacology , Pyrrolidines/chemistry , Pyrrolidines/pharmacology , Valine/analogs & derivatives , Administration, Oral , Animals , Dogs , Protease Inhibitors/chemical synthesis , Pyrrolidines/chemical synthesis , Rats , Valine/chemical synthesis , Valine/chemistry , Valine/pharmacology
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