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Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles

Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles

  1. ThirdEyeFloond
    Bioorganic & Medicinal Chemistry Letters
    Volume 18, Issue 15, 1 August 2008, Pages 4267-4274

    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.

    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.
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