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

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。

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.