SYNTHESIS AND ANTIAGGREGANT ACTIVITY OF 2-CYCLOALKYLAMINO-5-THIENYL- AND-5-FURYL-6H-1,3,4-THIADIAZINES / Chupakhin O. N.,Sidorova L. P.,Perova N. M.,Rusinov V. L.,Vasil'eva T. M.,Makarov V. A. // PHARMACEUTICAL CHEMISTRY JOURNAL. - 2011. - V. 45, l. 5. - P. 270-274.

ISSN/EISSN:

0091-150X / нет данных

Type:

Article

Abstract:

A series of new 5-(thienyl-2)-, 5-(furyl-2)-, and 5-(thienyl-3)-1,3,4-thiadiazine derivatives have been synthesized using methods based on the cyclocondensation of alpha-bromoacetylthiophenes or alpha-bromo-2-acetylfurans with 4-substituted thiosemicarbazides. The effects of the synthesized compounds on human platelet aggregation in vitro and on rabbit platelet aggregation ex vivo have been studied. The most active 5-(thienyl-2)-1,3,4-thiadiazines inhibit human platelet aggregation induced by ADP and arachidonic acid in a broad concentration range. These compounds have good potential as emergency drugs for the treatment and prophylaxis of infarction and stroke.

Author keywords:

synthesis; 1,3,4-thiadiazines; platelet aggregation 2,2-DIOXIDES; AGGREGATION

DOI:

нет данных

Web of Science ID:

ISI:000297597600003

Соавторы в МНС:

Другие поля

Поле	Значение
Month	AUG
Publisher	SPRINGER
Address	233 SPRING ST, NEW YORK, NY 10013 USA
Language	English
Keywords-Plus	2,2-DIOXIDES; AGGREGATION
Research-Areas	Pharmacology \& Pharmacy
Web-of-Science-Categories	Chemistry, Medicinal; Pharmacology \& Pharmacy
Author-Email	vlapp@isnet.ru protein7@rambler.ru
ORCID-Numbers	Makarov, Vladimir/0000-0002-2922-3246
Funding-Acknowledgement	Russian Foundation for Basic Research {[}08-03-12068-ofi]
Funding-Text	The work was supported financially by the Russian Foundation for Basic Research (Grant 08-03-12068-ofi).
Number-of-Cited-References	13
Usage-Count-Last-180-days	1
Usage-Count-Since-2013	5
Journal-ISO	Pharm. Chem. J.
Doc-Delivery-Number	855WS