New amino acid esters of salicylanilides active against MDR-TB and other microbes
Language English Country France Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
20937542
DOI
10.1016/j.ejmech.2010.09.040
PII: S0223-5234(10)00688-4
Knihovny.cz E-resources
- MeSH
- Amino Acids chemistry MeSH
- Anti-Bacterial Agents chemical synthesis chemistry pharmacology MeSH
- Antifungal Agents chemical synthesis chemistry pharmacology MeSH
- Bacteria drug effects MeSH
- Esters chemistry MeSH
- Extensively Drug-Resistant Tuberculosis microbiology MeSH
- Fungi drug effects MeSH
- Microbial Sensitivity Tests MeSH
- Molecular Structure MeSH
- Tuberculosis, Multidrug-Resistant microbiology MeSH
- Drug Design MeSH
- Salicylanilides chemical synthesis chemistry pharmacology MeSH
- Stereoisomerism MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Amino Acids MeSH
- Anti-Bacterial Agents MeSH
- Antifungal Agents MeSH
- Esters MeSH
- Salicylanilides MeSH
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).
References provided by Crossref.org
Antibacterial activity of salicylanilide 4-(trifluoromethyl)-benzoates
Antifungal Activity of Salicylanilides and Their Esters with 4-(Trifluoromethyl)benzoic Acid
In vitro antibacterial and antifungal activity of salicylanilide benzoates
Antimycobacterial activity of salicylanilide benzenesulfonates
