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首页> 外文期刊>Chemistry: A European journal >Protease Catalysis Mediated by a Substrate Mimetic: A Novel Enzymatic Approach to the Synthesis of Carboxylic Acid Amides
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Protease Catalysis Mediated by a Substrate Mimetic: A Novel Enzymatic Approach to the Synthesis of Carboxylic Acid Amides

机译：底物模拟物介导的蛋白酶催化：一种新型的羧酸酰胺合成酶方法

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摘要

We present a protease-based method for the coupling of non-coded and non-amino-acid derived amines with carboxy components. The key feature of this approach is the combination of the substrate-mimetic strategy with the ability of the cysteine protease clostripain to accept a wide spectrum of amines. Firstly, we tested the use of the 4-guanidinophenyl ester leaving group to mediate acceptance of noncoded and non-amino-acid-derived acyl residues. This employed #beta#-amino acid and simple carboxylic acid moieties as acyl donors, and several amino acid and peptide units as acyl acceptors. The study was completed by the use of non-amino-acid-derived acyl acceptors comprising simple amines, amino alcohols, and diamines. The results indicate that the approach presented is a useful strategy for the synthesis of peptide isosteres, peptide analogues, and organic amides. These last open a new range of synthetic applications of proteases completely beyond peptide synthesis, achieving efficient and selective acylations of non-amino-acid-derived amines under extraordinarily mild reaction conditions.
机译：我们提出了一种基于蛋白酶的非编码和非氨基酸衍生的胺与羧基成分偶联的方法。该方法的关键特征是模拟底物的策略与半胱氨酸蛋白酶Clostripain接受多种胺类的能力的结合。首先，我们测试了使用4-胍基苯基酯离去基团来介导接受非编码和非氨基酸衍生的酰基残基。该方法使用＃β＃-氨基酸和简单的羧酸部分作为酰基供体，并使用多个氨基酸和肽单元作为酰基受体。该研究是通过使用非氨基酸衍生的酰基受体（包括简单的胺，氨基醇和二胺）完成的。结果表明，所提出的方法是合成肽等排物，肽类似物和有机酰胺的有用策略。这些最后打开了蛋白酶合成的新应用范围，完全超出了肽的合成范围，在异常温和的反应条件下实现了非氨基酸衍生的胺的有效和选择性的酰化作用。

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