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Sci. Pharm. 2019, 87(1), 7; https://doi.org/10.3390/scipharm87010007

Cardioprotective Activity of Some 2-Arylimino-1,3-Thiazole Derivatives

1
Department of General, Bioinorganic, Physical and Colloidal Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010 Lviv-10, Ukraine
2
Department of Medicinal Chemistry, National University of Pharmacy, Pushkinska 53, 61002 Kharkiv, Ukraine
3
National T.G. Shevchenko University “Chernigiv Kollegium”, Hetmana Polubotka 53, 14013 Chernihiv, Ukraine
4
Department of Pharmaceutical, Organic and Bioorganic Chemistry (I.D.), Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010, Lviv-10, Ukraine
5
Department for Pharmacology of effector organs and systems SI “Institute of Pharmacology and Toxocology NAMS Ukraine”, A. Cedrika 14, 03057 Kyiv, Ukraine
*
Author to whom correspondence should be addressed.
Received: 12 February 2019 / Revised: 12 March 2019 / Accepted: 13 March 2019 / Published: 18 March 2019
(This article belongs to the Special Issue Heterocyclic Chemistry in Drug Design)
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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. View Full-Text
Keywords: Hantzsch reaction; 1,3-thiazole derivatives; cardioprotective activity Hantzsch reaction; 1,3-thiazole derivatives; cardioprotective activity
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MDPI and ACS Style

Drapak, I.; Perekhoda, L.; Demchenko, N.; Suleiman, M.; Rakhimova, M.; Demchuk, I.; Taran, S.; Seredynska, N.; Gerashchenko, I. Cardioprotective Activity of Some 2-Arylimino-1,3-Thiazole Derivatives. Sci. Pharm. 2019, 87, 7.

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