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  • Title: Design, synthesis, and pharmacological evaluation of highly potent and selective dipeptidyl peptidase-4 inhibitors.
    Author: Jiang T, Zhou Y, Zhu J, Chen Z, Sun P, Zhang Q, Wang Z, Shao Q, Jiang X, Li B, Wang H, Zhu W, Shen J.
    Journal: Arch Pharm (Weinheim); 2015 Jun; 348(6):399-407. PubMed ID: 25871012.
    Abstract:
    The optimization of a series of fused β-homophenylalanine inhibitors of dipeptidyl peptidase-4 (DPP-4) is described. Modification on the P2-binding moiety of 6 (IC50 = 10 nM) led to the discovery of β-homophenylalanine derivatives containing pyrrolidin-2-ylmethyl amides. The introduction of a sulfamine in the meta position of the phenyl ring improved the potency against DPP-4 (6-12-fold increase). Compound 14k showed DPP-4 inhibitory activity with an IC50 value of 0.87 nM. Meanwhile, in vivo experiments exhibited that 14h had an efficiency comparable to sitagliptin at the dose of 10 mg/kg.
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