Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists

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• 作者：Suk Youn Kang ; Sung-Han Lee ; Hee Jeong Seo ; Myung Eun Jung ; Kwangwoo Ahn ; Jeongmin Kim ; Jinhwa Lee
• 关键词：Rimonabant ; Anti-obesity ; Cannabinoid receptor antagonist ; Tetrazole
• 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 April 2008
• 卷：18
• 期：7
• 页码：2385-2389
• 文件大小：133 K

摘要

Cannabinoid CB1 receptors have been the focus of extensive studies since the first clinical results of rimonabant (SR141716) for the treatment of obesity and related metabolic disorders were reported in 2001. To further evaluate the properties of CB receptors, we have designed a new series of tetrazole-biarylpyrazoles. The various analogues were efficiently prepared and bio-assayed for binding to cannabinoid CB1 receptor. Six of the new compounds which displayed high in vitro CB1 binding affinities were assayed for binding to CB2 receptor. Noticeably, cyclopentyl-tetrazole (9a) demonstrated good binding affinity and selectivity for CB1 receptor (IC₅₀ = 11.6 nM and CB2/CB1 = 366).