4-甲氧基-1,3-苯二甲酸二苯酯类化合物的合成及其体外抗血小板聚集活性

Synthesis and in vitro activities on anti-platelet aggregation of bis-phenyl-4-methoxyisophthalate compounds

摘要: 以化合物4-甲氧基-1,3-苯二甲酸二苯酯（PO1）为先导化合物，合成了13个4-甲氧基-1,3-苯二甲酸二苯酯类化合物（PO1~PO13），其中8个化合物(PO6~PO13）未见文献报道。目标化合物结构已经由¹H NMR，IR，MS确证，并对各化合物进行了体外抗血小板聚集活性实验。活性测试结果表明，以上化合物均具有不同程度的抗血小板聚集活性；在4个引入-NO的化合物中，有3个化合物的抗血小板聚集活性明显增强；苯基上引入-CH₃的位置和个数对抗血小板聚集活性的影响很小。

Abstract: To search for new anti-platelet aggregation agents,13 target compounds (PO1-PO13) were designed and synthesized with diphenyl 4-methoxyisophthalate as the lead compound.Within this series of compounds,8 compounds (PO6-PO13) have not been reported before and their structures were confirmed by ¹H NMR，IR and MS.Anti-platelet aggregation activities of the target compounds were evaluated.It was found that all of the synthesized compounds possessed anti-platelet aggregation activities.3 compounds with nitroso group showed significantly enhanced anti-platelet aggregation activity.The location and numbers of substituted methyl groups had little effect on anti-platelet aggregation activities.