Esfahanizadeh Marjan, Mohebbi Shohreh, Dasht Bozorg Behnam, Amidi Salimeh, Gudarzi Ali, Ayatollahi Seyed Abdolmajid, Kobarfard Farzad
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.
Department of Medicinal Chemistry, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
Iran J Pharm Res. 2015 Spring;14(2):417-27.
A series of novel 2-aminopyrimidine and 2-Substituted-4,6-diaminopyrimidine derivatives have been synthesized and their antiplatelet aggregation activities were assessed against ADP and arachidonic acid-induced platelet aggregation in human plasma using light transmission aggregometry. Among the tested derivatives, compounds Ia, Ib, IB and II16 exhibited the highest antiplatelet aggregation activity (36.75, 72.4, 62.5 and 80 µM). None of the compounds showed satisfactory activity against the aggregation induced by ADP but acceptable activities were observed against the aggregation induced by arachidonic acid. 2- aminopyrimidines were more active than 4,6- diaminopyrimidines in this respect.
合成了一系列新型的2-氨基嘧啶和2-取代-4,6-二氨基嘧啶衍生物，并使用透光率聚集测定法评估了它们对人血浆中ADP和花生四烯酸诱导的血小板聚集的抗血小板聚集活性。在测试的衍生物中，化合物Ia、Ib、IB和II16表现出最高的抗血小板聚集活性（36.75、72.4、62.5和80μM）。没有一种化合物对ADP诱导的聚集表现出令人满意的活性，但对花生四烯酸诱导的聚集观察到了可接受的活性。在这方面，2-氨基嘧啶比4,6-二氨基嘧啶更具活性。
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