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New amino acid esters of salicylanilides active against MDR-TB and other microbes

Martin Krátký, Jarmila Vinšová, Vladimír Buchta, Kata Horvati, Szilvia Bösze, Jiřina Stolaříková

. 2010 ; 45 (12) : 6106-6113.

Jazyk angličtina Země Francie

Typ dokumentu časopisecké články, práce podpořená grantem

Perzistentní odkaz   https://www.medvik.cz/link/bmc12026737

Grantová podpora
NS10367 MZ0 CEP - Centrální evidence projektů

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).

Citace poskytuje Crossref.org

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