Synthesis and platelet aggregation inhibitory activity of 4,5-bis(substituted)-1,2,3-thiadiazoles

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Abstract
Routine screening of compounds for inhibition of collagen-induced human platelet aggregation in vitro revealed 4,5-bis-(4-methoxyphenyl)-1,2,3-thiadiazole was active and it represents the first example of a 1,2,3-thiadiazole with possible antithrombotic activity. In order to develop a structure-activity relationship for this heterocycle, a number of new 4(5)-mono- and -disubstituted 1,2,3-thiadiazoles were synthesized. These were tested in the screen and a number of additional active compounds were found. The most active compounds were those in which the heterocycle was substituted with benzene rings possessing P electron-donating groups.

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