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
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
收藏
页码:351 / 354
页数:4
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