778639-32-0Relevant academic research and scientific papers
Discovery of a new class of ghrelin receptor antagonists
Mihalic, Jeffrey T.,Kim, Yong-Jae,Lizarzaburu, Mike,Deignan, Jeff,Wanska, Malgorzata,Yu, Ming,Fu, Jiasheng,Chen, Xi,Zhang, Alex,Connors, Richard,Liang, Lingming,Lindstrom, Michelle,Ma, Ji,Tang, Liang,Dai, Kang,Li, Leping,Chen, Xiaoqi
scheme or table, p. 2046 - 2051 (2012/04/17)
A series of benzodiazepine antagonists of the human ghrelin receptor GHSR1a were synthesized and their antagonism and metabolic stability were evaluated. The potency of these analogs was determined using a functional aequorin (Euroscreen) luminescent assay measuring the intracellular Ca2+ concentration, and their metabolic stability was measured using an in vitro rat and human S9 hepatocyte assay. These efforts led to the discovery of a potent ghrelin antagonist with good rat pharmacokinetic properties.
Substituted benzofused heterocycles
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Page/Page column 39; 40, (2008/06/13)
The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for example, for the treatment and prevention of obesity, obesity-related disorders and eating disorders.
