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拉罗丁衍生物的抗菌活性药物筛选。

Drug screening of rhodanine derivatives for antibacterial activity.

机构信息

School of Chemistry & Physics, University of KwaZulu-Natal, Westville Campus, Durban, South Africa.

Department of Chemistry, GITAM Institute of Sciences, GITAM University, Visakhapatnam, India.

出版信息

Expert Opin Drug Discov. 2020 Feb;15(2):203-229. doi: 10.1080/17460441.2020.1696768. Epub 2019 Nov 28.

Abstract

: Bacteriological infections are a major risk to human health. These include all hospital and public-acquired infections. In drug discovery, rhodanines are privileged heterocyclic frameworks. Their derivatives possess strong anti-bacterial activity and some of them have shown potent activity against multidrug-resistant pathogens, both under and conditions. To treat multi-drug resistant pathogens, the development of novel potent drugs, with superior anti-bacterial efficacy, is paramount. One avenue which shows promise is the design and development of novel rhodanines.: This review summarizes the status on rhodanine-based derivatives and their anti-bacterial activity, based on published research over the past six years. Furthermore, to facilitate the design of novel derivatives with improved functions, their structure-activity relationships are assessed with reference to their efficacy as anti-bacterial agents and their toxicity.: The pharmacological activity of molecules bearing a rhodanine scaffold needs to be very critically assessed in spite of considerable information available from various biological evaluations. Although, some data on structure-activity relationship frameworks is available, information is not adequate to optimize the efficacy of rhodanine derivatives for different applications.

摘要

细菌感染对人类健康构成重大威胁。这些感染包括所有医院获得性感染和公共获得性感染。在药物发现中,硫代氨基甲酸酯是一种特权杂环框架。它们的衍生物具有很强的抗菌活性,其中一些在和条件下对多种耐药病原体都表现出很强的活性。为了治疗多药耐药病原体,开发具有更高抗菌功效的新型有效药物至关重要。有前途的途径之一是设计和开发新型硫代氨基甲酸酯。

本综述总结了过去六年中基于硫代氨基甲酸酯衍生物及其抗菌活性的研究现状。此外,为了设计具有更好功能的新型衍生物,参考其作为抗菌剂的功效和毒性评估了它们的结构-活性关系。

尽管从各种生物学评估中可以获得相当多的信息,但仍需要非常仔细地评估带有硫代氨基甲酸酯支架的分子的药理活性。尽管已经有一些关于构效关系框架的信息,但这些信息还不足以优化硫代氨基甲酸酯衍生物在不同应用中的功效。

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