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Bioorg Med Chem Lett. 2010 Nov 15;20(22):6785-9. doi: 10.1016/j.bmcl.2010.08.126. Epub 2010 Aug 31.

Expansion of SAR studies on triaryl bis sulfone cannabinoid CB2 receptor ligands.

Author information

1
Department of Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA. ling.tong@spcorp.com

Abstract

We report further expansion of the structure activity relationship (SAR) on the triaryl bis sulfone class of compounds (I), which are potent CB(2) receptor ligands with excellent selectivity over the CB(1) receptor. This study was extended to B ring changes, followed by simultaneous optimization of the A-, B-, and C-rings. Compound 42 has excellent CB(2) potency, selectivity and rat exposure.

PMID:
20850969
DOI:
10.1016/j.bmcl.2010.08.126
[Indexed for MEDLINE]

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