Synthesis of a Conformationally Fixed Bicyclomarin Derivative.

IF 3.4 4区医学 Q2 CHEMISTRY, MEDICINAL

ChemMedChem Pub Date : 2025-09-03 DOI:10.1002/cmdc.202500493

Jennifer Greve, Alexander F Kiefer, Uli Kazmaier

引用次数: 0

Abstract

Based on an X-ray structure of cyclomarin bound to ClpC1, a new conformationally fixed, bicyclic cyclomarin derivative is synthesized in an effort to enhance antituberculosis activity. The synthesis of the linear heptapeptide and the two macrolactamizations proceed smoothly. Only the very last synthetic step, the cleavage of a benzyl ether, provides a low yield. Despite the successful synthesis, the resulting bicyclic compound shows reduced activity compared to cyclomarin.

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一种构象固定的双环香素衍生物的合成。

根据环香素与ClpC1结合的x射线结构，合成了一种新的构象固定的双环环香素衍生物，以增强其抗结核活性。线性七肽的合成和两个大内酰胺化过程顺利进行。只有合成的最后一步，即苯醚的裂解，产率很低。尽管成功合成，所得到的双环化合物的活性低于环脲素。

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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来源期刊

ChemMedChem 医学-药学

CiteScore

6.70

自引率

2.90%

发文量

280

审稿时长

1 months

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