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Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.

Authors :
Lavey BJ
Kozlowski JA
Shankar BB
Spitler JM
Zhou G
Yang DY
Shu Y
Wong MK
Wong SC
Shih NY
Wu J
McCombie SW
Rizvi R
Wolin RL
Lunn CA
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jul 01; Vol. 17 (13), pp. 3760-4. Date of Electronic Publication: 2007 Apr 10.
Publication Year :
2007

Abstract

Structure-activity relationship on our recently reported triaryl bis-sulfone class of cannabinoid-2 (CB2) receptor selective inverse agonists was explored. Modifications to the methane sulfonamide, substitutions to B and C phenyl rings, and replacements of the C-ring were investigated. A compound with excellent CB2 activity, selectivity for CB2 over CB1, and in vivo plasma levels was identified.

Details

Language :
English
ISSN :
0960-894X
Volume :
17
Issue :
13
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
17466519
Full Text :
https://doi.org/10.1016/j.bmcl.2007.04.028