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  • Title: Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
    Author: Yu M, Lizarzaburu M, Beckmann H, Connors R, Dai K, Haller K, Li C, Liang L, Lindstrom M, Ma J, Motani A, Wanska M, Zhang A, Li L, Medina JC.
    Journal: Bioorg Med Chem Lett; 2010 Mar 01; 20(5):1758-62. PubMed ID: 20137933.
    Abstract:
    Piperazine-bisamide analogs were discovered as partial agonists of human growth hormone secretagogue receptor (GHSR) in a high throughput screen. The partial agonists were optimized for potency and converted into antagonists through structure-activity relationship (SAR) studies. The efforts also led to the identification of potent antagonist with favorable PK profile suitable as a tool compound for in vivo studies.
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