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Merck

Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Bioorganic & medicinal chemistry letters (2004-02-26)
Charles G Caldwell, Ping Chen, Jiafang He, Emma R Parmee, Barbara Leiting, Frank Marsilio, Reshma A Patel, Joseph K Wu, George J Eiermann, Aleksandr Petrov, Huaibing He, Kathryn A Lyons, Nancy A Thornberry, Ann E Weber
摘要

Amides derived from fluorinated pyrrolidines and 4-substituted cyclohexylglycine analogues have been prepared and evaluated as inhibitors of dipeptidyl dipeptidase IV (DP-IV). Analogues which incorporated (S)-3-fluoropyrrolidine showed good selectivity for DP-IV over quiescent cell proline dipeptidase (QPP). Compound 48 had good pharmacokinetic properties and was orally active in an oral glucose tolerance test in lean mice.

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Sigma-Aldrich
(R)-(-)-3-氟吡咯烷盐酸盐, 97%
Sigma-Aldrich
(S)-(+)-3-氟吡咯烷盐酸盐, 97%