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Bioorg Med Chem Lett. 2007 Jul 1;17(13):3760-4. Epub 2007 Apr 10.

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

Author information

1
Department of Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA. brian.lavey@spcorp.com <brian.lavey@spcorp.com>

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.

PMID:
17466519
DOI:
10.1016/j.bmcl.2007.04.028
[Indexed for MEDLINE]

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