论文部分内容阅读
High anti-thrombotic activity of aminoacid modified tetrahydro-b-carbolines was generally correlated with a small proximity of the side chain of the aminoacid residue to the carboline-cycle.This paper explored that the aromatization of the tetrahydro-b-carboline-cycle of N-(1-methyl-b-tetrahydrocarboline-3-carbonyl)-NO-(aminoacid-acyl)-hydrazines leaded to N-(1-methyl-b-carboline-3-carbonyl)-NO-(aminoacid-acyl)-hydrazines and decreased the proximity of the side chain of the aminoacid residue to the carboline-cycle.The in vitro activities of inhibiting pig platelet aggregation induced by PAF, ADP, and AA, as well as the in vivo anti-thrombotic activities of inhibiting rat thrombosis of these aromatized derivatives were generally higher than that of N-(1-methyl-b-tetrahydrocarboline-3-carbonyl)-NO-(aminoacid-acyl)-hydrazines.The understanding was also obtained from the 3D QSAR analysis.