摘要
目的：根据ＲＧＤ肽及目前活性较好的非肽类纤维蛋白原受体拮抗剂的结构特点，设计、合成一系列有抗血小板聚集活性的化合物。方法：以酪氨酸及对硝基苯甲酸等为主要原料经多步合成，对所得化合物用比浊法测定在１×１０－６ｍｏｌ·Ｌ－１时对体外血小板聚集的抑制率。结果：合成了１８个Ｎ取代Ｏ对甲脒苯胺基羰甲基Ｌ酪氨酸甲酯类化合物（Ｉａ～ｒ），均为新化合物。结论：其中１０个化合物（Ｉａ，ｆ，ｇ，ｉ～ｍ，ｑ，ｒ）显示一定的活性，活性最高的（Ｉｇ）抑制率达６４％。
AIM: To design and synthesize a class of compounds with inhibitory action upon ADPinduced platelet aggregation according to both the ArgGlyAsp(RGD) sequence and the nonpeptide fibrinogen receptor antagonists that have been reported. METHODS: Tyrosine and 4nitrobenzoic acid were used as the major reactants to obtain the target compounds by multistep synthesis. Turbidometric technique was used to assess the inhibitory effects in vitro at 110-6 molL-1. RESULTS: Eighteen compounds of NsubstitutedO(4aminoiminomethylphenylamino)carbonylmethylLtyrosine methyl ester were synthesized, ten ( THZIa,f,g,im,q,r ) of them showed inhibitory action at the above concentrations while Ig with inhitory rate of 64% is the most potent one. CONCLUSION: All of the eighteen compounds are new compounds, and most of them showed antiaggregation action on platelet richplasma.
出处
《药学学报》
CAS
CSCD
北大核心
1999年第6期428-433,共6页
Acta Pharmaceutica Sinica
关键词
抗血栓剂
Ia-r
酪氨酸甲酯类
纤维蛋白原
nonpeptide fibrinogen receptor antagonists
design
synthesis
NsubstitutedO(4aminoiminomethylphenylamino)carbonylmethylLtyrosine methyl ester
antiaggregation action
