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|Title:||Cardioprotective Activity of Some 2-Arylimino-1,3-Thiazole Derivatives|
|Authors:||Drapak, I. V.|
Perekhoda, L. O.
Suleiman, M. M.
Rakhimova, M. V.
Taran, S. G.
Seredynska, N. M.
Перехода, Л. О.
Сулейман, М. М.
Рахімова, М. В.
Драпак, И. В.
Драпак, І. В.
Рахимова, М. В.
Таран, С. Г.
Серединська, Н. М.
|Keywords:||Hantzsch reaction;1,3-thiazole derivatives;cardioprotective activity|
|Bibliographic description (Ukraine):||Cardioprotective Activity of Some 2-Arylimino-1,3-Thiazole Derivatives / I. Drapak, L. Perekhoda, N. Demchenko, M. Suleiman, M. Rakhimova, I. Demchuk, S. Taran, N. Seredynska, I. Gerashchenko // Sci. Pharm. – 2019. – № 87 (7). – Р. 1-8.|
|Abstract:||The article presents the synthesis of 2-arylimino-4-methyl-2,3-dihydro-1,3-thiazoles via Hantzsch reaction of thioureas and 3-chloropentane-2,4-dione or ethyl 2-chloro-3-oxobutanoate. The structure of synthesized compounds was confirmed by LCMS, 1H, and 13C NMR spectra. Cardioprotective activity of synthesized thiazole derivatives were studied in vitro on the isolated rings of the thoracic aorta of laboratory rats. Based on pharmacological studies, the tested compounds possessed a moderate to high cardioprotective effect. A prospective 1-[2-(4-methoxyphenylimino)-4-methyl-3-(4-methylpiperazine-1-yl)-2,3-dihydro-1,3-thiazole-5-yl] ethan-1-one hydrochloride 4c was identified. The mentioned compound has delayed the development of constrictor responses of isolated rings of the thoracic rat aorta and exceeds the activity of L-carnitine by 18.2% and meldonium by 12.9%. The compound 4c may be proposed as a potential cardioprotective agent for in-depth pharmacological studies.|
|Description:||The purpose of the project was the search for new safe and effective biologically active substances with a cardioprotective action among 1,3-thiazole derivatives. Despite a large number of publications, there is practically no information in the literature on the physical, chemical, and biological properties of compounds bearing the combination of different heterocyclic core nuclei such as piperazine, morpholine, and 1,3-thiazole cores in one molecule. Since in current medicine there are some examples of the successful use of drugs based on these heterocycles, we considered it expedient to combine these known important structures in one molecule|
|Appears in Collections:||Наукові публікації кафедри медичної хiмiї|
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