SYNTHESIS AND ANALGESIC ACTIVITIES OF SOME (4-SUBSTITUTED PHENYL-1-PIPERAZINYL)ALKYL 2-AMINOBENZOATES AND 2-AMINONICOTINATES

被引：21

作者：

MANOURY, PM ^{[1
]}

DUMAS, AP ^{[1
]}

NAJER, H ^{[1
]}

BRANCENI, D ^{[1
]}

PROUTEAU, M ^{[1
]}

LEFEVREBORG, FM ^{[1
]}

机构：

[1] SYNTHOLAB,DEPT BIOL RES,F-75621 PARIS 13,FRANCE

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 05期

关键词：

D O I：

10.1021/jm00191a017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of (4-substituted phenyl-l-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates has been prepared and screened for analgesic and antiinflammatory properties in mice and rats. The tabulated results reveal several 2-(4-substituted phenyl-1-piperazinyl)ethyl 2-(7-or 8-substituted 4-quinolinylamino)benzoates to be six to nine times more potent analgesics than the reference compounds (glafenine and aminopyrine) and to possess minor antiinflammatory activity. Compound 45, 2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl 2-[[7-(trifluoromethyl)-4-quinolinyl]amino]benzoate (antrafenine), showed marked analgesic activity, long duration of action, and excellent tolerance in pharmacological and toxicological studies, as well as in clinical trials. © 1979, American Chemical Society. All rights reserved.

引用

页码：554 / 559

页数：6