1261296-11-0Relevant articles and documents
New amino acid esters of salicylanilides active against MDR-TB and other microbes
Krátky, Martin,Vin?ová, Jarmila,Buchta, Vladimír,Horvati, Kata,B?sze, Szilvia,Stola?íková, Ji?ina
experimental part, p. 6106 - 6113 (2011/01/13)
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).