摘要 : It is known that the Arg-Gly-Asp sequence in the fibrinogen molecule is key in binding to the receptors on the surface of platelets. We searched for the compounds which were able to inhibit the binding and synthesized the followin... 展开 It is known that the Arg-Gly-Asp sequence in the fibrinogen molecule is key in binding to the receptors on the surface of platelets. We searched for the compounds which were able to inhibit the binding and synthesized the following analogs of this sequence: 2-acetoxybenzoyl-Arg-beta Ala-Asp, 4-piperidinecarbonyl-beta Ala-Asp, and 4-aminobezoyl-beta Ala-Asp. These compounds were shown to inhibit the platelets aggregation in a different degree. The 2-acetoxybenzoyl-Arg-beta Ala-Asp analog demonstrated the highest inhibitory activity. A decrease in the expression of the CD62p and CD63 markers on platelets was also found after the action of the Arg-Gly-Asp analogs, confirming the ability of these compounds to block the fibrinogen binding sites for the GP IIb/IIIa glycoprotein receptors. 收起