Syntheses and SH-enzyme inhibitory activities of new epoxysuccinic acid piperazine derivatives against mu-calpain and cathepsin B.

Drug design and discovery Pub Date : 1999-08-01

J Inoue, Y Yoshida, M Nakamura, Y S Cui, Y Nagao

引用次数: 0

Abstract

New chiral epoxysuccinic acid derivatives 5 approximately 23 bearing various amino acids and N-substituted piperazines were synthesized to evaluate their inhibitory activities against mu-calpain and cathepsin B. After screening these compounds, 1-[(2S,3S)-epoxysuccinyl-L-leucyl]-4-(2-chlorophenyl)piperazine 9 proved to exhibit fairly strong inhibitory activity against both cysteine proteases. L-Valyl derivative 19 exhibited selective inhibitory activity against cathepsin B in comparison with that against mu-calpain.

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新型环氧琥珀酸哌嗪衍生物的合成及其对钙蛋白酶和组织蛋白酶B的sh酶抑制活性。

本文合成了约23个含不同氨基酸和n -取代哌嗪的手性环氧琥珀酸衍生物5，以评价其对mucalpain和cathepsin b的抑制活性。经筛选，1-[(2S,3S)-环氧琥珀酰-l -亮基]-4-(2-氯苯基)哌嗪9对这两种半胱氨酸蛋白酶均表现出较强的抑制活性。L-Valyl衍生物19对组织蛋白酶B表现出选择性抑制活性，而对mu-calpain则表现出选择性抑制活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Drug design and discovery

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