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ID: ALA1147603

Journal: Bioorg Med Chem Lett

Title: Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Authors: Caldwell CG, Chen P, He J, Parmee ER, Leiting B, Marsilio F, Patel RA, Wu JK, Eiermann GJ, Petrov A, He H, Lyons KA, Thornberry NA, Weber AE.

Abstract: 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.

CiteXplore: 14980678

DOI: 10.1016/j.bmcl.2003.12.040