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  • Title: New amino acid esters of salicylanilides active against MDR-TB and other microbes.
    Author: Krátký M, Vinšová J, Buchta V, Horvati K, Bösze S, Stolaříková J.
    Journal: Eur J Med Chem; 2010 Dec; 45(12):6106-13. PubMed ID: 20937542.
    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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