Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

Autor: Saleem, Ahmad, William N, Washburn, Andres S, Hernandez, Sharon, Bisaha, Khehyong, Ngu, Wei, Wang, Mary Ann, Pelleymounter, Daniel, Longhi, Neil, Flynn, Anthony V, Azzara, Kenneth, Rohrbach, James, Devenny, Suzanne, Rooney, Michael, Thomas, Susan, Glick, Helen, Godonis, Susan, Harvey, Hongwei, Zhang, Brian, Gemzik, Evan B, Janovitz, Christine, Huang, Lisa, Zhang, Jeffrey A, Robl, Brian J, Murphy
Rok vydání: 2016
Předmět:
Zdroj: Journal of medicinal chemistry. 59(19)
ISSN: 1520-4804
Popis: The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficacious antiobesity agent with a relatively clean in vitro and in vivo safety profile.
Databáze: OpenAIRE