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ID: ALA1147816

Journal: Bioorg Med Chem Lett

Title: Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.

Authors: Tsai TY, Coumar MS, Hsu T, Hsieh HP, Chien CH, Chen CT, Chang CN, Lo YK, Wu SH, Huang CY, Huang YW, Wang MH, Wu HY, Lee HJ, Chen X, Chao YS, Jiaang WT.

Abstract: A series of substituted pyrrolidine-2,4-dicarboxylic acid amides were synthesized as potential antidiabetic agents, and many of them showed good in vitro DPP-IV inhibition (IC50 = 2-250 nM) with selectivity over DPP-II, DPP8, and FAP enzymes. Selected compounds 8c and 11a showed in vivo plasma DPP-IV inhibition after oral administration in Wistar rats.

CiteXplore: 16581245

DOI: 10.1016/j.bmcl.2006.03.037