Synthesis and antiaggregant activity of 2-cycloalkylamino-5-thienyl- and -5-furyl-6H-1,3,4-thiadiazines

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 α-bromoacetylthiophenes or α-bromo-2-acetylfurans with 4-substituted thiosemicarbazides. The effects of the synthesized compounds on hum...

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Bibliographic Details
Published in:Pharmaceutical chemistry journal 2011-08, Vol.45 (5), p.270, Article 270
Main Authors: Chupakhin, O. N., Sidorova, L. P., Perova, N. M., Rusinov, V. L., Vasil’eva, T. M., Makarov, V. A.
Format: Article
Language:English
Subjects:
Cardiovascular agents
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
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Summary: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 α-bromoacetylthiophenes or α-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.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-011-0614-y