2. Academic Validation
  3. Expansion of SAR studies on triaryl bis sulfone cannabinoid CB2 receptor ligands

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

  • Bioorg Med Chem Lett. 2010 Nov 15;20(22):6785-9. doi: 10.1016/j.bmcl.2010.08.126.
Ling Tong 1,  B B Shankar,  Lei Chen,  Razia Rizvi,  Joseph Kelly,  Eric Gilbert,  Chunli Huang,  De-Yi Yang,  Joseph A Kozlowski,  N-Y Shih,  W Gonsiorek,  R William Hipkin,  Asra Malikzay,  Charles A Lunn,  Daniel J Lundell
Affiliations

Affiliation

  • 1 Department of Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033-0539, USA. [email protected]
PMID: 20850969 DOI: 10.1016/j.bmcl.2010.08.126
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.

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