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Novel benzimidazole derivatives as selective CB2 agonists.

Authors :
Pagé D
Balaux E
Boisvert L
Liu Z
Milburn C
Tremblay M
Wei Z
Woo S
Luo X
Cheng YX
Yang H
Srivastava S
Zhou F
Brown W
Tomaszewski M
Walpole C
Hodzic L
St-Onge S
Godbout C
Salois D
Payza K
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jul 01; Vol. 18 (13), pp. 3695-700. Date of Electronic Publication: 2008 May 22.
Publication Year :
2008

Abstract

The preparation and evaluation of a novel class of CB2 agonists based on a benzimidazole moiety are reported. They showed binding affinities up to 1nM towards the CB2 receptor with partial to full agonist potencies. They also demonstrated good to excellent selectivity (>1000-fold) over the CB1 receptor.

Details

Language :
English
ISSN :
1464-3405
Volume :
18
Issue :
13
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
18522867
Full Text :
https://doi.org/10.1016/j.bmcl.2008.05.073