The discovery of novel indole-2-carboxamides as cannabinoid CB(1) receptor antagonists

Phillip M Cowley; James Baker; David R Barn; Kirsteen I Buchanan; Ian Carlyle; John K Clark; Thomas R Clarkson; Maureen Deehan; Darren Edwards; Richard R Goodwin; David Jaap; Yasuko Kiyoi; Chris Mort; Ronald Palin; Alan Prosser; Glenn Walker; Nick Ward; Grant Wishart; Trevor Young

doi:10.1016/j.bmcl.2010.10.104

The discovery of novel indole-2-carboxamides as cannabinoid CB(1) receptor antagonists

Bioorg Med Chem Lett. 2011 Jan 1;21(1):497-501. doi: 10.1016/j.bmcl.2010.10.104. Epub 2010 Oct 26.

Affiliation

¹ Department of Chemistry, MSD, Newhouse, Lanarkshire ML1 5SH, UK. phillip.cowley@merck.com

PMID: 21075628
DOI: 10.1016/j.bmcl.2010.10.104

Abstract

The discovery and structure-activity relationship of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 26i was found to be a high potency, selective cannabinoid CB(1) antagonist.

MeSH terms

Amides / chemical synthesis
Amides / chemistry*
Amides / pharmacokinetics
Animals
Dogs
Drug Evaluation, Preclinical
Indoles / chemical synthesis
Indoles / chemistry*
Indoles / pharmacokinetics
Male
Mice
Models, Molecular
Rats
Rats, Wistar
Receptor, Cannabinoid, CB1 / antagonists & inhibitors*
Receptor, Cannabinoid, CB1 / metabolism
Structure-Activity Relationship

Substances

Amides
Indoles
Receptor, Cannabinoid, CB1