Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands

被引：14

作者：

Lavey, Brian J.

Kozlowski, Joseph A.

Shankar, Bandarpalle B.

Spitler, James M.

Zhou, Guowei

Yang, De-Yi

Shu, Youlieng

Wong, Michael K. C.

Wong, Shing-Chun

Shih, Neng-Yang

Wu, Jie

McCombie, Stuart W.

Rizvi, Razia

Wolin, Ronald L.

Lunn, Charles A.

机构：

[1] Schering Plough Res Inst, Dept Chem, Kenilworth, NJ 07033 USA

[2] Schering Plough Res Inst, Dept Immunol, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 13期

关键词：

CB2 receptor ligands; inverse agonists; cannabinoid receptors; cannabinoid-2; CB2; anti-inflammatory;

D O I：

10.1016/j.bmcl.2007.04.028

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity relationship on our recently reported triaryl bis-sulfone class of cannabinoid-2 (C132) receptor selective inverse agonists was explored. Modifications to the methane sulfonamide, substitutions to B and C phenyl rings, and replacements of the C-ring were investigated. A compound with excellent C132 activity, selectivity for C132 over CB I, and in vivo plasma levels was identified. (c) 2007 Elsevier Ltd. All rights reserved.

引用

收藏

页码：3760 / 3764

页数：5

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