α2 adrenoceptor agonists as potential analgesic agents.: 1.: (Imidazolylmethyl)oxazoles and -thiazoles

被引：23

作者：

Boyd, RE ^{[1
]}

Press, JB ^{[1
]}

Rasmussen, CR ^{[1
]}

Raffa, RB ^{[1
]}

Codd, EE ^{[1
]}

Connelly, CD ^{[1
]}

Bennett, DJ ^{[1
]}

Kirifides, AL ^{[1
]}

Gardocki, JF ^{[1
]}

Reynolds, B ^{[1
]}

Hortenstein, JT ^{[1
]}

Reitz, AB ^{[1
]}

机构：

[1] RW Johnson Pharmaceut Res Inst, Drug Discovery Div, Spring House, PA 19477 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1999年 / 42卷 / 25期

关键词：

D O I：

10.1021/jm990005a

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of (imidazolylmethyl)oxazoles and -thiazoles were prepared and evaluated as alpha(2) adrenoceptor agonists. These compounds were also tested in in vivo paradigms that are predictive of analgesic activity. Variations in both the imidazole and thiazole portions of the molecule were investigated. Some of the more potent compounds such as 22, 26, 45, and 53 displayed at receptor binding in the 10-20 nM range and also had significant, antinociceptive activity in the mouse abdominal irritant test (MAIT).

引用

页码：5064 / 5071

页数：8

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