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    J Med Chem. 2011 Jan 27;54(2):510-24. doi: 10.1021/jm101016w. Epub 2010 Dec 27.

    Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.

    Zhang Z, Wallace MB, Feng J, Stafford JA, Skene RJ, Shi L, Lee B, Aertgeerts K, Jennings A, Xu R, Kassel DB, Kaldor SW, Navre M, Webb DR, Gwaltney SL.

    Source

    Takeda San Diego, Inc., 10410 Science Center Drive, San Diego, California 92121, United States.

    Abstract

    The discovery of two classes of heterocyclic dipeptidyl peptidase IV (DPP-4) inhibitors, pyrimidinones and pyrimidinediones, is described. After a single oral dose, these potent, selective, and noncovalent inhibitors provide sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes. Compounds 13a, 27b, and 27j were selected for development.

    PMID:
    21186796
    [PubMed - indexed for MEDLINE]

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