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水蛭素Ｃ端肽段为抗凝的活性部位〔１〕．为了进行构效关系的研究，构建Ｃ端肽段类似物的化学库，首先利用同步多中心合成技术合成了７种水蛭素Ｃ端类似物．经ＨＰＬＣ制备纯化，纯度在９６％以上．电喷雾质谱确认了合成肽的分子量．用新鲜人血浆，进行了凝血酶原激酶时间（ＡＰＴＴ）、凝血酶时间（ＴＴ）及凝血酶原时间（ＰＴ）测定．显示水蛭素羧端２０个氨基酸残基肽片是抗凝活性必需的基本骨架．其中应当包含封闭凝血酶催化位点和阴离子结合位点的特异结合序列以及保持两者间多功能性的连接桥．
Hirudin C-terminal peptide anticoagulant active site [1]. In order to study the structure-activity relationship, a chemical library of C-terminal peptide analogues was constructed. Seven kinds of hirudin C terminal analogs were synthesized by synchronous multi-center synthesis. Purification by HPLC, purity above 96%. Electrospray mass spectrometry confirmed the molecular weight of the synthetic peptide. Prothrombin time (APTT), thrombin time (TT) and prothrombin time (PT) were measured with fresh human plasma. Showing hirudin carboxy terminal 20 amino acid residues Peptide anticoagulant activity is essential for the basic skeleton. Which should contain specific binding sequences that block the catalytic and anionic thrombin binding sites and bridges that maintain the versatility between the two.