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  • Title: 3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes.
    Author: Coumar MS, Chang CN, Chen CT, Chen X, Chien CH, Tsai TY, Cheng JH, Wu HY, Han CH, Wu SH, Huang YW, Hsu T, Hsu LJ, Chao YS, Hsieh HP, Jiaang WT.
    Journal: Bioorg Med Chem Lett; 2007 Mar 01; 17(5):1274-9. PubMed ID: 17194587.
    Abstract:
    Based on the structures of NVP-DPP728 (1) and NVP-LAF237 (Vildagliptin, 2), three series of DPP-IV inhibitors were synthesized by linking substituted anilines, benzylamines, and phenylethylamines to (2S)-cyanopyrrolidine through a linker. More than 20 compounds were evaluated for their in vitro DPP-IV inhibition and selectivity profile over DPP-II, DPP8, and FAP enzymes. Selected compounds 5f and 7i showed in vivo plasma DPP-IV inhibition and inhibited glucose excursion in OGTT after oral administration in Wistar rats. Compound 5f (DPP-IV IC50 = 116 nM) has the potential for development as antidiabetic agent.
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