SYNTHESES OF N-SUBSTITUTED 2(3,4)-PYRIDYLCARBOXYLIC ACID HYDRAZIDES WITH ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY

被引：34

作者：

REDDA, K ^{[1
]}

CORLETO, LA ^{[1
]}

KNAUS, EE ^{[1
]}

机构：

[1] UNIV ALBERTA,FAC PHARM & PHARMACEUT SCI,EDMONTON T6G 2N8,ALBERTA,CANADA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 09期

关键词：

D O I：

10.1021/jm00195a013

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A group of N-substituted 2(3, 4)-pyridylcarboxylic acid hydrazides were synthesized to investigate the effects that changes in functionality on the terminal hydrazide nitrogen have on analgesic and antiinflammatory activities. The most active analgesic-antiinflammatory compound was l-(2-pyridylcarbonyl)-2-(2-pyridyl)hydrazine (10a), which was much more potent than dextropropoxyphene and caused a 100% inhibition of carrageenan-induced paw edema up to 5 h. Pyridylcarbonylhydrazides 5a, 8, and 10c exhibited analgesic activity similar to dextropropoxyphene. Although 10b was an inactive analgesic agent, it exhibited antiinflammatory activity similar to 10a. © 1979, American Chemical Society. All rights reserved.

引用

页码：1079 / 1082

页数：4

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