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Hybridization Approach to Drug Discovery Inhibiting Mycobacterium tuberculosis-An Overview
Current Topics in Medicinal Chemistry ( IF 3.4 ) Pub Date : 2021-03-31 , DOI: 10.2174/1568026620666200819151342
Daniele Zampieri 1 , Maria G Mamolo 1
Affiliation  

Tuberculosis is one of the top 10 causes of death worldwide and the leading cause of death from a single infectious agent, mainly due to Mycobacterium tuberculosis (MTB). Recently, clinical prognoses have worsened due to the emergence of multi-drug resistant (MDR) and extensive-drug resistant (XDR) tuberculosis, which lead to the need for new, efficient and safe drugs. Among the several strategies, polypharmacology could be considered one of the best solutions, in particular, the multitarget directed ligands strategy (MTDLs), based on the synthesis of hybrid ligands acting against two targets of the pathogen. The framework strategy comprises linking, fusing and merging approaches to develop new chemical entities. With these premises, this review aims to provide an overview of the recent hybridization approach, in medicinal chemistry, of the most recent and promising multitargeting antimycobacterial candidates.



中文翻译:

抑制结核分枝杆菌药物发现的杂交方法-概述

结核病是全球 10 大死亡原因之一,也是单一传染源死亡的主要原因,主要是由结核分枝杆菌 (MTB) 引起。最近,由于耐多药(MDR)和广泛耐药(XDR)结核病的出现,临床预后恶化,这导致需要新的、有效的和安全的药物。在几种策略中,多药理学可以被认为是最好的解决方案之一,特别是多靶点定向配体策略 (MTDL),它基于对病原体的两个靶标起作用的杂合配体的合成。该框架战略包括链接、融合和合并方法以开发新的化学实体。有了这些前提,本综述旨在概述最近在药物化学中的杂交方法,

更新日期:2021-05-26
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