Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a Novel, Acyclic Cannabinoid-1 Receptor Inverse Agonist for the Treatment of Obesity

Autor:	Xinchun Tong, Yue Feng, Lauren P. Shearman, William K. Hagmann, Koppara Samuel, Jing Chen Xiao, Shrenik K. Shah, Hongbo Qi, Junying Wang, Sanjeev Kumar, Kimberly Rosko, Tung M. Fong, Wenji Yin, Ping Liu, D. Sloan Stribling, Linus S. Lin, Alison M. Strack, Chun-Pyn Shen, Julie Lao, Donald J. Marsh, James P. Jewell, Lex H.T. Van der Ploeg, Thomas J. Lanza, Mark T. Goulet, Suoyu S. Xu
Rok vydání:	2006
Předmět:	Trifluoromethyl Stereochemistry Propanamide Chemical synthesis chemistry.chemical_compound Taranabant chemistry In vivo Amide Drug Discovery medicine Molecular Medicine Inverse agonist Receptor medicine.drug
Zdroj:	Journal of Medicinal Chemistry. 49:7584-7587
ISSN:	1520-4804 0022-2623
Popis:	The discovery of novel acyclic amide cannabinoid-1 receptor inverse agonists is described. They are potent, selective, orally bioavailable, and active in rodent models of food intake and body weight reduction. A major focus of the optimization process was to increase in vivo efficacy and to reduce the potential for formation of reactive metabolites. These efforts led to the identification of compound 48 for development as a clinical candidate for the treatment of obesity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::703cbf2be468c2f985946aa5e12958db https://doi.org/10.1021/jm060996+ Zobrazit plný text záznamu