1221403-24-2Relevant articles and documents
Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity
Yu, Ming,Lizarzaburu, Mike,Beckmann, Holger,Connors, Richard,Dai, Kang,Haller, Katrin,Li, Cong,Liang, Lingming,Lindstrom, Michelle,Ma, Ji,Motani, Alykhan,Wanska, Malgorzata,Zhang, Alex,Li, Leping,Medina, Julio C.
scheme or table, p. 1758 - 1762 (2010/07/05)
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.