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近年来,1,2,3-和 1,2,4-三唑杂合体作为抗菌剂及其 SAR 的研究进展:批判性评价。

Recent advances in 1,2,3- and 1,2,4-triazole hybrids as antimicrobials and their SAR: A critical review.

机构信息

Key Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Hubei Engineering Research Center for Advanced Fine Chemicals, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei 430205, China.

Key Laboratory for Green Chemical Process of Ministry of Education, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Hubei Engineering Research Center for Advanced Fine Chemicals, School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei 430205, China.

出版信息

Eur J Med Chem. 2023 Nov 5;259:115603. doi: 10.1016/j.ejmech.2023.115603. Epub 2023 Jul 16.

DOI:10.1016/j.ejmech.2023.115603
PMID:37478558
Abstract

With the widespread use and sometimes even abuse of antibiotics, the problem of bacterial resistance to antibiotics has become very serious, and it is posing a great threat to global health. Therefore, development of new antibiotics is imperative. Triazoles are five-membered, nitrogen-containing aromatic heterocyclic scaffolds, with two isomeric forms, i.e. 1,2,3-triazole and 1,2,4-triazole. Triazole-containing compounds have a wide range of biological activities such as antibacterial, antifungal, anticancer, antioxidant, antitubercular, antimalarial, anti-HIV, anticonvulsant, anti-inflammatory, antiulcer, analgesic, and etc. The bioactivities and the diversity of triazole-containing drugs have attracted wide interest in these heterocycles. Various antibiotic triazole hybrids have been developed, and most of which have shown potent antimicrobial activities. In this review, we summarized the recent advances in triazole hybrids as potential antibacterial agents and their structure-activity relationships (SARs). The information gained through SAR studies will provide further insights into the development of new triazole antimicrobials.

摘要

随着抗生素的广泛应用,甚至有时滥用,细菌对抗生素的耐药性问题变得非常严重,对全球健康构成了巨大威胁。因此,开发新的抗生素是当务之急。三唑是一种含有五个氮原子的五元含氮芳香杂环骨架,有两种异构体,即 1,2,3-三唑和 1,2,4-三唑。含三唑的化合物具有广泛的生物活性,如抗菌、抗真菌、抗癌、抗氧化、抗结核、抗疟疾、抗 HIV、抗惊厥、抗炎、抗溃疡、止痛等。三唑类药物的生物活性和多样性引起了人们对这些杂环的广泛关注。已经开发了各种抗生素三唑杂合体,其中大多数表现出很强的抗菌活性。在这篇综述中,我们总结了作为潜在抗菌剂的三唑杂合体的最新进展及其结构-活性关系 (SAR)。通过 SAR 研究获得的信息将为开发新的三唑类抗菌药物提供进一步的见解。

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