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

Document Type: Research article

Authors

1 Department of medicinal chemistry, school of pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran. Central Research Laboratories, Shahid Beheshti University of Medical Sciences, Tehran, Iran

2 Department of medicinal chemistry, school of pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.

3 Department of medicinal chemistry, school of pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran

4 Department of medicinal chemistry, school of pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran Phytochemistry research center, Shahid Beheshti University of Medical Sciences, Tehran, Iran

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Abstract

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.

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