| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371652 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
We report further expansion of the structure activity relationship (SAR) on the triaryl bis sulfone class of compounds (I), which are potent CB2 receptor ligands with excellent selectivity over the CB1 receptor. This study was extended to B ring changes, followed by simultaneous optimization of the A-, B-, and C-rings. Compound 42 has excellent CB2 potency, selectivity and rat exposure.
Graphical abstractSAR exploration on triaryl bis sulfone A led us to structurally novel and diverse CB2 selective ligands B.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ling Tong, 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,