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

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 -bromoacetylthiophenes or -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.