Sulfamoyl benzamides as novel CB₂ cannabinoid receptor ligands

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• 作者：Karin Worm ; Q. Jean Zhou ; Christopher T. Saeui ; Rosalyn C. Green ; Joel A. Cassel ; Gabriel J. Stabley ; Robert N. DeHaven ; Nathalie Conway-James ; Christopher J. LaBuda ; Michael Koblish ; Patrick J. Littl
• 关键词：Cannabinoid CB₂ receptor ; Parallel synthesis ; Sulfamoyl benzamides ; Structure– ; activity relationship ; Antiallodynic activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 May 2008
• 卷：18
• 期：9
• 页码：2830-2835
• 文件大小：219 K

摘要

Sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Starting from a screening hit 8 that had modest affinity for the cannabinoid CB₂ receptor, a parallel synthesis approach and initial SAR are described, leading to compound 27 with 120-fold functional selectivity for the CB₂ receptor. This compound produced robust antiallodynic activity in rodent models of postoperative pain and neuropathic pain without traditional cannabinergic side effects.