Abstract：
A series of stilbene analogues, in which a phenyl ring was replaced by the pyridazin-3(2H)-one nucleus, was designed and synthesized to be explored as platelet aggregation inhibitors. The proposed stilbene-pyridazinone hybrids were successfully obtained from simple starting materials and by Wittig\'s reaction. Most of the target compounds displayed improved in vitro activity in comparison with the standard drug, resveratrol, highlighting as the most potent the analogues 10d and 10e, with inhibition percentages of 94.15 % at 100 µM and 100 % at 50 µM, respectively. The pharmacokinetic and toxicity (ADME/T) properties of the novel hybrids were also estimated with the SwissADME and ProTox-II web servers.
摘要：
一系列的二苯乙烯类似物，其中一个苯环被吖嗪-3（2H）-一核取代，被设计和合成作为血小板聚集抑制剂进行探索。从简单的起始材料和Wittig's反应成功地获得了提出的二苯乙烯-吖嗪酮杂化物。与标准药物相比，大多数目标化合物显示出改善的体外活性，白藜芦醇,突出显示10d和10e类似物是最有效的，100µM时的抑制百分比为94.15%，50µM时的抑制百分比为100%，分别。还使用SwissADME和ProTox-II网络服务器估算了新型杂种的药代动力学和毒性（ADME/T）特性。
