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  • Title: Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.
    Author: Wallace MB, Feng J, Zhang Z, Skene RJ, Shi L, Caster CL, Kassel DB, Xu R, Gwaltney SL.
    Journal: Bioorg Med Chem Lett; 2008 Apr 01; 18(7):2362-7. PubMed ID: 18346892.
    Abstract:
    A novel series of non-covalent, benzimidazole-based inhibitors of DPP-4 has been developed from a small fragment hit using structure-based drug design. A highly versatile synthetic route was created for the development of SAR, which led to the discovery of potent and selective inhibitors with excellent pharmaceutical properties.
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