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    Bioorg Med Chem Lett. 2009 Mar 15;19(6):1797-801. doi: 10.1016/j.bmcl.2009.01.058. Epub 2009 Jan 23.

    Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors.

    Rew Y, McMinn DL, Wang Z, He X, Hungate RW, Jaen JC, Sudom A, Sun D, Tu H, Ursu S, Villemure E, Walker NP, Yan X, Ye Q, Powers JP.

    Source

    Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.

    Abstract

    Discovery and optimization of a piperidyl benzamide series of 11beta-HSD1 inhibitors is described. This series was derived from a cyclohexyl benzamide lead structures to address PXR selectivity, high non-specific protein binding, poor solubility, limited in vivo exposure, and in vitro cytotoxicity issues observed with the cyclohexyl benzamide structures. These efforts led to the discovery of piperidyl benzamide 15 which features improved properties over the cyclohexyl benzamide derivatives.

    PMID:
    19217779
    [PubMed - indexed for MEDLINE]

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