作为特异性凝血酶抑制剂的Nα-芳基磺酰基-ω-脒基苯基-α-氨基烷基-羧酸酰胺

N alpha-arylsulfonyl-omega-amidinophenyl-alpha-aminoalkyl-carboxylic acid amides as specific thrombin inhibitors.

作者信息

Stürzebecher J

出版信息

Folia Haematol Int Mag Klin Morphol Blutforsch. 1982;109(1):83-8.

Abstract

Structure-activity relationships for the inhibition of thrombin and trypsin by N alpha-substituted amidinophenyl-alpha-aminoalkylcarboxylic acid amides are presented. Secondary cyclic amides of N alpha-substituted 4-amidinophenylalanine and 2-amino-5-(4-amidinophenyl)valeric acid were found to be potent and specific inhibitors of thrombin, whereas trypsin was inhibited strongly by primary amides of 2-amino-4-(4-amidinophenyl) butyric acid. For this type of inhibitor the carbon amide structure seems to play a decisive role in the enzyme-inhibitor interaction.

摘要

本文介绍了Nα-取代脒基苯基-α-氨基烷基羧酸酰胺对凝血酶和胰蛋白酶的抑制作用的构效关系。发现Nα-取代的4-脒基苯丙氨酸和2-氨基-5-(4-脒基苯基)戊酸的仲环酰胺是凝血酶的强效和特异性抑制剂，而2-氨基-4-(4-脒基苯基)丁酸的伯酰胺对胰蛋白酶有强烈抑制作用。对于这类抑制剂，碳酰胺结构似乎在酶-抑制剂相互作用中起决定性作用。

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N alpha-arylsulfonyl-omega-amidinophenyl-alpha-aminoalkyl-carboxylic acid amides as specific thrombin inhibitors.作为特异性凝血酶抑制剂的Nα-芳基磺酰基-ω-脒基苯基-α-氨基烷基-羧酸酰胺

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