Title:Hybridization Approach to Drug Discovery Inhibiting Mycobacterium tuberculosis-An Overview
Volume: 21
Issue: 9
Author(s): Daniele Zampieri*Maria G. Mamolo
Affiliation:
- Department of Chemical and Pharmaceutical Sciences, P.le Europa 1, University of Trieste, Trieste 34127,Italy
Keywords:
Antimycobacterial, Cytotoxicity, Hybridization, MIC, MDR, MTDLs, Tuberculosis.
Abstract: 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.