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    Bioorg Med Chem Lett. 2008 Aug 1;18(15):4267-74. doi: 10.1016/j.bmcl.2008.06.096. Epub 2008 Jul 3.

    Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.

    DiMauro EF, Buchanan JL, Cheng A, Emkey R, Hitchcock SA, Huang L, Huang MY, Janosky B, Lee JH, Li X, Martin MW, Tomlinson SA, White RD, Zheng XM, Patel VF, Fremeau RT Jr.

    Source

    Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA. edimauro@amgen.com

    Erratum in

    • Bioorg Med Chem Lett. 2009 Jan 1;19(1):284.
    • Bioorg Med Chem Lett. 2008 Sep 15;18(18):5156.

    Abstract

    Structural modifications to the central portion of the N-arylamide oxadiazole scaffold led to the identification of N-arylpiperidine oxadiazoles as conformationally constrained analogs that offered improved stability and comparable potency and selectivity. The simple, modular scaffold allowed for the use of expeditious and divergent synthetic routes, which provided two-directional SAR in parallel. Several potent and selective agonists from this novel ligand class are described.

    PMID:
    18640038
    [PubMed - indexed for MEDLINE]

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