815650-69-2Relevant academic research and scientific papers
Identification of novel bivalent mimetics of annonaceous acetogenins via a scaffold-hopping strategy
Liu, Yanghan,Liu, Yongqiang,Li, Zhen,Zhou, Guang-Biao,Yao, Zhu-Jun,Jiang, Sheng
, p. 1650 - 1653 (2014/04/17)
A series of novel bivalent mimetics of annonaceous acetogenins have been designed, synthesized, and evaluated. Among these, compound 7 bearing a homopiperazine ring in the middle region exhibited more potent growth inhibitory activity and higher selectivity against cancer cells over normal cells by comparison with AA005. This work indicates that modification of the middle piperazine ring is a useful optimizing tool for the simplified acetogenin mimetics.
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.
