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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Current Frontiers

Hybridization Approach to Drug Discovery Inhibiting Mycobacterium tuberculosis-An Overview

Author(s): Daniele Zampieri* and Maria G. Mamolo

Volume 21 , Issue 9 , 2021

Published on: 19 August, 2020

Page: [777 - 788] Pages: 12

DOI: 10.2174/1568026620666200819151342

Price: $65


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.

Keywords: Antimycobacterial, Cytotoxicity, Hybridization, MIC, MDR, MTDLs, Tuberculosis.

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