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.
From: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. linus_lin@merck.com
Journal of medicinal chemistry
- Publish Date: Dec 2006
- ISSN: 0022-2623
- Volume: 49
- Issue: 26
- Pages: 7584-7
- Medium: Print
- Language: English
- Citation (JAMA): Lin Linus S, Lanza Thomas J, Jewell James P, et al. 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.. J. Med. Chem. Dec 2006;49:7584-7
Abstract
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.
Mesh Headings (Keywords): Animals, Anti-Obesity Agents, Body Weight, Cannabinoids, Cyclic AMP, Eating, Humans, Liver, Microsomes, Obesity, Rats, Receptor, Cannabinoid, CB1, Receptor, Cannabinoid, CB2
Check for Full Text / PubMed Unique Identifier (PMID): 17181138
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