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Updated: Jun 8, 2026

Assay Development for High-Throughput Drug Screening Against Mycobacteria
Published on: October 25, 2024
New amino acid esters of salicylanilides active against MDR-TB and other microbes
Martin Krátký1, Jarmila Vinšová, Vladimír Buchta
1Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, and Department of Clinical Microbiology, University Hospital, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.
Abstract:
Eleven halogenated (S)-2-(phenylcarbamoyl)phenyl 2-acetamido-3-phenylpropanoates (3a-3k) were designed and synthesized as potential antimicrobial agents. They were evaluated in vitro against some mycobacterial, bacterial and fungal strains. These compounds were active against drug-sensitive and atypical mycobacterial strains with general MIC values from 0.25 to 16 μmol/L. The most active compounds were (S)-4-chloro-2-(4-(trifluoromethyl)phenylcarbamoyl)phenyl 2-acetamido-3-phenylpropanoate (3i) and (S)-4-bromo-2-(4-(trifluoromethyl)phenylcarbamoyl)phenyl 2-acetamido-3-phenylpropanoate (3k) which exhibited activity against MDR and XDR-TB strains with MICs from 1 to 2 μmol/L. 3k was shown to be less cytotoxic with higher IC50. Some compounds exhibited low MICs on Gram-positive bacteria (MICs≥0.98 μmol/L) and on fungi (MICs≥3.9 μmol/L).
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