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

被引：7

作者：

Drapak, Iryna ^{[1
]}

Perekhoda, Lina ^{[2
]}

Demchenko, Natalya ^{[3
]}

Suleiman, Marharyta ^{[2
]}

Rakhimova, Maryna ^{[2
]}

Demchuk, Inna ^{[4
]}

Taran, Svitlana ^{[2
]}

Seredynska, Nataliya ^{[5
]}

Gerashchenko, Inna ^{[5
]}

机构：

[1] Danylo Halytsky Lviv Natl Med Univ, Dept Gen Bioinorgan Phys & Colloidal Chem, Pekarska 69, UA-79010 Lvov 10, Ukraine

[2] Natl Univ Pharm, Dept Med Chem, Pushkinska 53, UA-61002 Kharkov, Ukraine

[3] Natl TG Shevchenko Univ Chernigiv Kollegium, Hetmana Polubotka 53, UA-14013 Chernihiv, Ukraine

[4] Danylo Halytsky Lviv Natl Med Univ, Dept Pharmaceut Organ & Bioorgan Chem ID, Pekarska 69, UA-79010 Lvov 10, Ukraine

[5] Inst Pharmacol & Toxocol NAMS Ukraine, Dept Pharmacol Effector Organs & Syst SI, A Cedrika 14, UA-03057 Kiev, Ukraine

来源：

SCIENTIA PHARMACEUTICA | 2019年 / 87卷 / 01期

关键词：

Hantzsch reaction; 1; 3-thiazole derivatives; cardioprotective activity; AGENTS; PREVENTION; DRUG;

D O I：

10.3390/scipharm87010007

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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, H-1, and C-13 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.

引用

页数：8

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