2-arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists.: Part 1:: Discovery of CB2 receptor selective compounds

被引：31
作者：
Kai, Hiroyuki
Morioka, Yasuhide
Murashi, Takarni
Morita, Koichi
Shinonome, Satorni
Nakazato, Hitoshi
Kawamoto, Keiko
Hanasaki, Kohji
Takahashi, Furniyo
Mihara, Shin-ichi
Arai, Tohko
Abe, Kohji
Okabe, Hirosh
Baba, Takahiko
Yoshikawa, Takayoshi
Takenaka, Hideyuki
机构：
[1] Shionogi & Co Ltd, Shionogi Res Labs, Fukushima Ku, Osaka 5530002, Japan
[2] Shionogi & Co Ltd, Dev Res Labs, Toyonaka, Osaka 5610825, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 14期
关键词：
1,3-thiazine; cannabinoid receptor agonist; CB2 receptor selective; CB1; CB2; pain; structure-activity relationship;
D O I：
10.1016/j.bmcl.2007.04.093
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
2-Arylimino-5,6-dihydro-4H-1,3-thiazines have been identified as a novel class of cannabinoid agonists. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure-activity relationships led to the discovery of potent agonists of CB2 receptor. The most potent compound 13 displays K-i values of > 5000 and 9 nM to CB1 and CB2 receptors, respectively. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4030 / 4034
页数：5
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