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  • Title: Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors.
    Author: Li N, Wang LJ, Jiang B, Guo SJ, Li XQ, Chen XC, Luo J, Li C, Wang Y, Shi DY.
    Journal: Bioorg Med Chem Lett; 2018 Jul 01; 28(12):2131-2135. PubMed ID: 29773502.
    Abstract:
    A series of novel pyrimidinedione derivatives were designed and evaluated for in vitro dipeptidyl peptidase-4 (DPP-4) inhibitory activity and in vivo anti-hyperglycemic efficacy. Among them, the representative compounds 11, 15 and 16 showed excellent inhibitory activity of DPP-4 with IC50 values of 64.47 nM, 188.7 nM and 65.36 nM, respectively. Further studies revealed that compound 11 was potent in vivo hypoglycemic effect. The structure-activity relationships of these pyrimidinedione derivatives had been discussed, which would be useful for developing novel DPP-4 inhibitors as treating type 2 diabetes.
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