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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.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2016 Oct 13; Vol. 59 (19), pp. 8848-8858. Date of Electronic Publication: 2016 Sep 15. - Publication Year :
- 2016
-
Abstract
- 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.
- Subjects :
- Animals
Anti-Obesity Agents pharmacokinetics
Anti-Obesity Agents pharmacology
Dogs
Halogenation
Humans
Macaca fascicularis
Male
Mice
Pyrimidines pharmacokinetics
Pyrimidines pharmacology
Rats
Receptors, Somatostatin metabolism
Structure-Activity Relationship
Anti-Obesity Agents chemistry
Anti-Obesity Agents therapeutic use
Obesity drug therapy
Pyrimidines chemistry
Pyrimidines therapeutic use
Receptors, Somatostatin antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 59
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 27564419
- Full Text :
- https://doi.org/10.1021/acs.jmedchem.6b00676