Synthesis and Biological Activity of Quinoline-2-Carboxylic Acid Aryl Esters and Amides

被引：8

作者：

Boyarshinov, V. D. ^{[1
]}

Mikhalev, A. I. ^{[1
]}

Yushkova, T. A. ^{[1
]}

Ukhov, S. V. ^{[1
]}

Kon'shina, T. M. ^{[1
]}

机构：

[1] Perm State Pharmaceut Acad, Minist Hlth Russia, 2 Polevaya St, Perm 614990, Russia

来源：

PHARMACEUTICAL CHEMISTRY JOURNAL | 2017年 / 51卷 / 05期

关键词：

quinoline-2-carboxylic acid; quinoline-2-carboxylic acid aryl esters; quinoline-2-carboxylic acid amides; anti-inflammatory activity; analgesic activity;

D O I：

10.1007/s11094-017-1613-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Derivatives of quinoline-4-carboxylic acid are known to possess anti-inflammatory and analgesic activity. However, structurally analogous amides and esters of quinoline-2-carboxylic acid are insufficiently studied. In the present work, esters and substituted amides of quinoline-2-carboxylic acid were prepared by reacting quinoline-2-carboxylic acid chloride with phenol or arylamine, respectively. The structures of the synthesized compounds were confirmed using spectroscopic data; the purities, TLC. The physicochemical properties of the target reaction products were determined. Animal experiments determined the anti-inflammatory and analgesic activities as compared with the standard drug diclofenac sodium. The developed method for synthesizing quinoline-2-carboxylic acid derivatives could be used in preparative organic chemistry to prepare potentially biologically active quinoline derivatives.

引用

页码：351 / 354

页数：4