| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375362 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
The triaryl bis-sulfone 1 was modified by converting the aryl A-ring to a piperidine ring. The piperidine ring was further elaborated to a spirocyclopropyl piperidine moiety. The effect on CB2 binding potency, rat calcium channel affinity, and CYP 2C9 inhibition is described.
Graphical abstractA-ring replacements of 1 were investigated leading to compound 53 which had good affinity for the human CB2 receptor, reduced affinity for the rat calcium channel, and an improved cytochrome P450 profile.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Eric J. Gilbert, Guowei Zhou, Michael K.C. Wong, Ling Tong, Bandarpalle B. Shankar, Chunli Huang, Joseph Kelly, Brian J. Lavey, Stuart W. McCombie, Lei Chen, Razia Rizvi, Youhao Dong, Youheng Shu, Joseph A. Kozlowski, Neng-Yang Shih, R. William Hipkin,