Synthesis and Antiplatelet Aggregation Activity Evaluation of some 2-Aminopyrimidine and 2-Substituted-4,6-diaminopyrimidine Derivatives

A series of novel 2-aminopyrimidine and 2-Substituted-4,6-diaminopyrimidine derivatives have been synthesized and their anti platelet aggregation activities were assessed against ADP and arachidonic acid- induced platelet aggregation in human plasma using light transmission aggregometry. None of the compounds showed satisfactory activity against the aggregation induced by ADP. However, satisfactory activities were observed in both groups against the aggregation induced by arachidonic acid. Comparing the overall results obtained for aminopyrimidines I and II indicates that 2-aminopyrimidines (I) were more active than 4,6-diaminopyrimidines (II). Among the tested derivatives, compounds Ia, Ib, IB and II16 exhibited the highest anti platelet aggregation activity (36.75, 72.4, 62.5 and 80 µM). Interestingly, compounds with fluorine substituent on phenyl ring (Ib, IB) were among the most active compounds.