Scientific journal
Fundamental research
ISSN 1812-7339
"Перечень" ВАК
ИФ РИНЦ = 1,798

SYNTHESIS AND BIOLOGICAL ACTIVITY QUINOLINE-2-CARBOXAMIDES

Boyarshinov V.D 1, Mikhalev A.I 1, Yushkova T.A 1, Konshina T.A 1, Ukhov S.V 1,
1 Perm State Pharmaceutical Academy
According to the literature data derivatives of quinoline-2-carboxylic acid include compounds exhibiting a different biological activity. In this work, substituted quinoline-2-carboxylic acid amides were synthesized in good yields by the reaction of the methyl quinoline-2-carboxylate with amines in ethylene glycol at 170–180 °C and quinoline-2-carboxylic (quinaldinic) acid chloride with amines in benzene at 50 °C. The structures of received compounds have been determined on the basic NMR 1H spectral data. Purity of the synthesized compounds was confirmed by thin layer chromatography data. Physico-chemical properties of the final products were determined. In animal studies, was determined anti-inflammatory and analgesic activity compared to standard drug: diclofenac sodium. Developed technique of synthesis of quinoline -2-carboxylic acids amides can be used in preparative organic chemistry for obtaining bioactive substances potentially quinoline series.
quinoline-2-carboxylic acid
quinoline-2-carboxamides
anti-inflammatory
analgesic activity.
1. Belenkij M.L., Jelementy kolichestvennoj ocenki farmakologicheskogo jeffekta, 2-e izd., L.: Medgiz, 1963. рр. 81–106.
2. Bojarshinov V.D., Mihalev A.I., Uhov S.V., Jushkova T.A., Mahmudov R.R. Sintez, svojstva i biologicheskaja aktivnost amidov piridin-2-karbonovoj kisloty // Fundamentalnye issledovanija 2014. Chast 3. no. 9. рр. 606–610.
3. Rukovodstvo po jeksperimentalnomu (doklinicheskomu) izucheniju novyh farmakologicheskih veshhestv / pod obshhej red. R.U. Habrieva. Izd. 2-e, pererab. i dop. / – M.: Medicina. 2005. 832 р.
4. Bobal P., Sujan J., Otevrel J., Imramovsky A., Padelkova Z., Jampilek J. Microwave-assisted synthesis of new substituted anilides of quinaldic acid // Molecules 2012. 17. рр. 1292–1306.
5. Gonec T., Bobal P., Sujan J., Pesko M., Guo J., Kralova K., Pavlacka L., Vesely L., Kreckova E., Kos J., Coffey A., Kollar P., Imramovsky A., Placek L., Jampilek J. Investigating the spectrum of biological activity of substituted quinoline-2-carboxamides and their isosteres // Molecules 2012. 17. рр. 613–644.

Библиографическая ссылка

Бояршинов В.Д., Михалев А.И., Юшкова Т.А., Коньшина Т.А., Ухов С.В., СИНТЕЗ И БИОЛОГИЧЕСКАЯ АКТИВНОСТЬ ХИНОЛИН-2-КАРБОКСАМИДОВ // Фундаментальные исследования. 2015. № 2-8. С. 1715-1719;
URL: https://fundamental-research.ru/en/article/view?id=37258 (дата обращения: 25.06.2026).