Synthesis, Characterization, and In Vitro Evaluation of New Amino‐Alcohol Quinolines as Promising Antimycobacterial Agents
Abstract
Nontuberculous mycobacteria (NTM) mainly Mycobacterium avium complex (MAC), are emerging pathogens responsible for pulmonary infections. Therefore, the effectiveness of the gold standard treatment is compromised by the emergence of intrinsic and acquired resistance of MAC. In this context, seventeen amino-alcohol quinolines as mefloquine analogs were developed as part of this work. Studies on the physicochemical properties, cytotoxicity and activity of these quinoline-based compounds, in relation to their structures, highlighted the important role of the trifluoromethyl and piperazine moieties. Thus, (R)-4c was identified as the most promising anti-MAC compound with the highest selectivity index value of 5.8. It was tested, in two-drug combinations, using a checkerboard assays with the standard antibiotics (clarithromycin, rifampicin and ethambutol), demonstrating an additive effect with each antibiotic of this gold standard treatment. These results confirm the potential of amino-alcohol quinolines as alternative of current anti-NTM agents.
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BibTeX
@article{charrier2026synthesis,
title = {{Synthesis, Characterization, and In Vitro Evaluation of New Amino‐Alcohol Quinolines as Promising Antimycobacterial Agents}},
author = {Elise Si Ahmed Charrier and François Peltier and Jean‐françois Raimbert and Marie Perret and Claire Andréjak and Alexandra Dassonville‐klimpt and Pascal Sonnet},
journal = {ChemMedChem},
year = {2026},
month = oct,
doi = {10.1002/cmdc.70543},
url = {https://u-picardie.hal.science/hal-05837552v1},
note = {CC BY 4.0},
}
RIS
TY - JOUR
TI - Synthesis, Characterization, and In Vitro Evaluation of New Amino‐Alcohol Quinolines as Promising Antimycobacterial Agents
AU - Elise Si Ahmed Charrier
AU - François Peltier
AU - Jean‐françois Raimbert
AU - Marie Perret
AU - Claire Andréjak
AU - Alexandra Dassonville‐klimpt
AU - Pascal Sonnet
PY - 2026
DA - 2026/10/22
JO - ChemMedChem
DO - 10.1002/cmdc.70543
UR - https://u-picardie.hal.science/hal-05837552v1
AB - Nontuberculous mycobacteria (NTM) mainly Mycobacterium avium complex (MAC), are emerging pathogens responsible for pulmonary infections. Therefore, the effectiveness of the gold standard treatment is compromised by the emergence of intrinsic and acquired resistance of MAC. In this context, seventeen amino-alcohol quinolines as mefloquine analogs were developed as part of this work. Studies on the physicochemical properties, cytotoxicity and activity of these quinoline-based compounds, in relation to their structures, highlighted the important role of the trifluoromethyl and piperazine moieties. Thus, (R)-4c was identified as the most promising anti-MAC compound with the highest selectivity index value of 5.8. It was tested, in two-drug combinations, using a checkerboard assays with the standard antibiotics (clarithromycin, rifampicin and ethambutol), demonstrating an additive effect with each antibiotic of this gold standard treatment. These results confirm the potential of amino-alcohol quinolines as alternative of current anti-NTM agents.
SN - 1860-7179
SN - 1860-7187
ER -