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  • Title: Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.
    Author: Liu KK, Cornelius P, Patterson TA, Zeng Y, Santucci S, Tomlinson E, Gibbons C, Maurer TS, Marala R, Brown J, Kong JX, Lee E, Werner W, Wenzel Z, Vage C.
    Journal: Bioorg Med Chem Lett; 2010 Jan 01; 20(1):266-71. PubMed ID: 19914063.
    Abstract:
    Based on our original pyrazine hit, CP-0809101, novel conformationally-restricted 5HT2c receptor agonists with 2-piperazin-azaindane scaffold were designed. Synthesis and structure-activity relationship (SAR) studies are described with emphasis on optimization of the selectivity against 5HT2a and 5HT2b receptors with excellent 2c potency. Orally-active and selective compounds were identified with dose-responsive in vivo efficacy in our pre-clinical food intake model.
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