糖蛋白（GP）IIb/IIIa拮抗剂的合成与活性

血小板凝聚最后的共同的一步是纤维蛋白原结合糖蛋白IIb/IIIa受体，因此GPII／IIIa受体拮抗剂应优于阻断其他单一途径的抗血小板药物。合成了13个化合物，其中4个化合物在体我活性上和模板化合物相当。

Synthesis and activity of glycoprotein IIb/IIIa antagonist

Platelet aggregation is a central event associated with arterial thrombus formation and is mediated by the binding of fibrinogen to its platelet membrane receptor of glycoprotein IIb/IIIa (GPIIb/IIIa ). This binding is the final common pathway that takes place during platelet activation regardless of the agonist involved (collagen, thrombin, etc ). Therefore, using GPIIb/IIIa antagonists is potentially superior to inhibition of individual platelet agonists. Based on the QSAR model and me too drug design principle, a series of new compounds were designed and synthesized through the change of the side chains of natural amino acids of sibrafiban and lamifiban, which used as model compounds. Four compounds showed activity comparable to that of the model compounds.