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药学学报  2015 

n,n'-二卤代苯基-4-甲氧基-1,3-苯二磺酰胺类化合物的设计、合成及体外抗血小板聚集活性评价

, PP. 185-190

Keywords: 合成,4-甲氧基-1,3-苯二磺酰胺,吡考他胺,利曲他班,抗血小板聚集

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Abstract:

依据药物化学结构设计中拼合和等排原则,拼合抗血小板聚集药物吡考他胺(picotamide)和利曲他班(linotroban)的结构,用磺酰基代替甲酰基,设计合成了n,n'-二卤代苯基-4-甲氧基-1,3-苯二磺酰胺系列化合物(4a~4m、5a~5n),各化合物的结构由ir、1hnmr和hr-ms光谱确证。以吡考他胺为阳性对照药,采用born比浊法检测目标化合物抗二磷酸腺苷(adp)诱导的体外抗血小板聚集活性,结果显示其中12个化合物(4b、4f、4l、5b、5d~5g、5j、5k、5m和5n)对adp诱导的血小板聚集的抑制活性优于阳性对照药吡考他胺。此外,初步探讨了目标化合物的构效关系。

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