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吲哚和吲唑类支架在抗菌剂中的应用:概述、合成及抗菌研究的最新进展。

Indole and Indoline Scaffolds in Antimicrobials: Overview, Synthesis and Recent Advances in Antimicrobial Research.

机构信息

Department of Pharmaceutical Science, School of Pharmacy, Southern Illinois University Edwardsville, Campus Box 2000, Edwardsville IL 62026, United States.

出版信息

Curr Med Chem. 2021;28(24):4828-4844. doi: 10.2174/0929867327666201102114923.

Abstract

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.

摘要

目前,抗生素耐药性传染病的大流行是一个日益严重的威胁。人们迫切需要新的抗生素和对抗抗生素耐药性的方法。这篇综述将重点介绍两种不同的优势骨架,即吲哚和吲哚啉,它们可作为新型抗菌化合物的有用核心。吲哚是许多已批准用于多种疾病状态的药物中的一种成分,最近因其作为对抗抗生素耐药菌(尤其是耐甲氧西林金黄色葡萄球菌 (MRSA))化合物的有用骨架而受到研究。吲哚啉是一种支架,历史研究和 FDA 批准的药物都明显较少,它在药物设计和开发方面引起了新的兴趣。近年来,已证明含吲哚啉的化合物具有抗菌活性,并且作为一种耐药性修饰剂 (RMA) 具有活性,可提高已知耐药性的现有抗生素治疗的有效性。

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