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

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...

Full description

Saved in:
Bibliographic Details
Published in:Scientia pharmaceutica 2019-03, Vol.87 (1), p.7-8
Main Authors: Drapak, Iryna, Perekhoda, Lina, Demchenko, Natalya, Suleiman, Marharyta, Rakhimova, Maryna, Demchuk, Inna, Taran, Svitlana, Seredynska, Nataliya, Gerashchenko, Inna
Format: Article
Language:English
Subjects:
Coronary vessels
Ethanol
Nitrogen
Systematic review
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:2218-0532
0036-8709
2218-0532
DOI:10.3390/scipharm87010007