肠肽A类似物的固相合成

IF 4.7 1区化学 Q1 CHEMISTRY, ORGANIC

Organic Letters Pub Date : 2026-10-14 DOI:10.1021/acs.orglett.6c04116

Karen D. Milewska,Fletcher M. Sharp,Lara R. Malins

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引用次数: 0

摘要

Enteropeptin A是一种具有独特的六元硫多肽核的天然产物。在这里，我们描述了一种固相肽合成（SPPS）兼容的方法，以肠肽a类似物为特征，具有简化的节氨酸基序。该策略采用了易于接近的构建块和高效的树脂组装。一个“从N到C”的变异，在节肢连锁的方向上不同，也很容易获得。总的来说，这项工作加速了对这类重要天然产物类似物的获取。

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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Solid-Phase Synthesis of Enteropeptin A Analogues

Abstract Enteropeptin A is a sactipeptide natural product featuring a unique six-membered thiomorpholine core. Herein, we describe a solid-phase peptide synthesis (SPPS)-compatible approach to enteropeptin A analogues featuring a simplified sactionine motif. The strategy employs a readily accessible building block and efficient on-resin assembly. A “N to C” variant, differing in the directionality of the sactionine linkage was also readily accessible. Collectively, this work accelerates access to analogues of this important class of natural products.

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来源期刊

Organic Letters 化学-有机化学

CiteScore

9.30

自引率

11.50%

发文量

1607

审稿时长

1.5 months

期刊介绍： Organic Letters invites original reports of fundamental research in all branches of the theory and practice of organic, physical organic, organometallic,medicinal, and bioorganic chemistry. Organic Letters provides rapid disclosure of the key elements of significant studies that are of interest to a large portion of the organic community. In selecting manuscripts for publication, the Editors place emphasis on the originality, quality and wide interest of the work. Authors should provide enough background information to place the new disclosure in context and to justify the rapid publication format. Back-to-back Letters will be considered. Full details should be reserved for an Article, which should appear in due course.