| 20137933 |
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: Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1758-62. Epub 2010 Jan 20.
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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