New Structure Activity Relationship Insight into the Role of the C-3 Extension on Rifamycin Antimycobacterial Activity.

IF 3.4 4区医学 Q2 CHEMISTRY, MEDICINAL

ChemMedChem Pub Date : 2025-09-22 DOI:10.1002/cmdc.202500673

Clinton G L Veale, Ewelina Smolarz, Aleksandra Leśniewska, Krystian Pyta, Piotr Przybylski

引用次数: 0

Abstract

Herein, the antimycobacterial screening of a series of rifamycin analogues, modified at their C-3 extension, is reported. Overall, these compounds display potent activity against a wild-type Mtb strain assayed in three different growth media. Several promising C-3 extensions are identified through this screen, with compounds featuring rigid tertiary alicyclic hydrazones displaying superior activity to amino compounds. In addition, a general correlative trend between logP and biological activity is observed. This study adds to the growing literature surrounding structure activity relationship pertaining the important C-3 extension of rifamycin, which in addition to a poorly understood role in target engagement, has utility for modulating physicochemical properties, a key condition in antimycobacterial drug discovery.

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新结构-活性关系对利福霉素抗细菌活性的影响

本文报道了一系列利福霉素类似物的抗细菌筛选，这些类似物在其C-3延伸处进行了修饰。总的来说，这些化合物在三种不同的培养基中对一种野生型结核分枝杆菌菌株显示出有效的活性。几个有希望的C-3扩展通过该筛选确定，具有刚性叔脂环腙的化合物显示优于氨基化合物的活性。此外，logP与生物活性之间存在普遍的相关趋势。这项研究增加了关于利福霉素重要的C-3延伸的结构活性关系的文献，除了在靶标结合中鲜为人知的作用外，它还具有调节物理化学性质的效用，这是抗真菌药物发现的关键条件。

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

期刊介绍： Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.