摘要
对新的抗生素和对抗抗生素耐药性的方法的需求是显而易见的。本文将重点介绍吲哚和吲哚啉这两种新型抗菌化合物的核心结构。吲哚是众多被批准用于治疗多种疾病的药物中的一种,最近人们对其作为化合物的母核的作用进行了研究,这些化合物对多重耐药菌具有抑菌活性,特别是对耐甲氧西林金黄色葡萄球菌(MRSA)。吲哚啉是一种具有较少历史研究及FDA批准的药物中间体成分,在药物设计和开发方面引起人们广泛的关注及研究兴趣。近年来,含吲哚类化合物已被证明具有抗菌活性以及作为耐药性修饰剂(RMA)的活性,其作用是提高目前已知有耐药性抗生素治疗的有效性。
关键词: 抗菌素、传染病、吲哚、吲哚类、抗生素耐药性、合成。
Current Medicinal Chemistry
Title:Indole and Indoline Scaffolds in Antimicrobials: Overview, Synthesis and Recent Advances in Antimicrobial Research
Volume: 28 Issue: 24
关键词: 抗菌素、传染病、吲哚、吲哚类、抗生素耐药性、合成。
摘要: At present, a pandemic of antibiotic-resistant infectious diseases is an evergrowing threat. The need for new antibiotics and ways to combat antibiotic resistance is glaring. This review will focus on two different privileged scaffolds, the indole and the indoline, as useful nuclei for novel antibacterial compounds. The indole, a moiety found in numerous approved drugs for many disease states, has recently been studied for its usefulness as a scaffold for compounds that have activity against antibiotic-resistant bacteria, especially against methicillin-resistant Staphylococcus aureus (MRSA). The indoline is a scaffold with significantly less historical studies and FDA-approved drugs and it has attracted new interest in drug design and development. In recent years, indoline-containing compounds have been shown to have antibacterial activity as well as activity as a resistance- modifying agent (RMA), which act to improve the effectiveness of current antibiotic therapies that have known resistance.
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Cite this article as:
Indole and Indoline Scaffolds in Antimicrobials: Overview, Synthesis and Recent Advances in Antimicrobial Research, Current Medicinal Chemistry 2021; 28 (24) . https://dx.doi.org/10.2174/0929867327666201102114923
DOI https://dx.doi.org/10.2174/0929867327666201102114923 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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