Salicylanilide N-monosubstituted carbamates: Synthesis and in vitro antimicrobial activity
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
26879856
DOI
10.1016/j.bmc.2016.02.004
PII: S0968-0896(16)30076-1
Knihovny.cz E-resources
- Keywords
- Antibacterial activity, Antifungal activity, In vitro activity, Salicylanilide carbamate, Staphylococcus aureus,
- MeSH
- Anti-Bacterial Agents chemical synthesis chemistry pharmacology MeSH
- Antifungal Agents chemical synthesis chemistry pharmacology MeSH
- Gram-Negative Bacteria drug effects MeSH
- Fungi drug effects MeSH
- Carbamates chemical synthesis chemistry pharmacology MeSH
- Microbial Sensitivity Tests MeSH
- Molecular Structure MeSH
- Salicylanilides chemical synthesis chemistry pharmacology 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
- Anti-Bacterial Agents MeSH
- Antifungal Agents MeSH
- Carbamates MeSH
- Salicylanilides MeSH
The research of innovative antimicrobial agents represents a cutting edge topic. Hence, we synthesized and characterised novel salicylanilide N-monosubstituted carbamates. Twenty compounds were evaluated in vitro against eight bacterial strains and eight fungal species. The lowest minimum inhibitory concentrations (MICs) were found to be ⩽0.49 μM. Genus Staphylococcus, including methicillin-resistant Staphylococcus aureus, and fungus Trichophyton mentagrophytes showed uniformly the highest rate of susceptibility, whilst Gram-negative bacteria and most of the fungi were less susceptible. A wide range of carbamates provided comparable or superior in vitro antimicrobial activity in comparison to established drugs. Interestingly, extended-spectrum β-lactamase producing strain of Klebsiella pneumoniae was inhibited with MICs starting from 31.25 μM. With respect to Staphylococci, 2-[(4-bromophenyl)carbamoyl]-4-chlorophenyl phenylcarbamate exhibited the lowest MIC values (⩽0.98 μM). 2-[(4-Bromophenyl)carbamoyl]-4-chlorophenyl benzylcarbamate showed the widest spectrum of antifungal action. The results indicate that some salicylanilide carbamates can be considered to be promising candidates for future investigation.
References provided by Crossref.org
2-Hydroxy-N-phenylbenzamides and Their Esters Inhibit Acetylcholinesterase and Butyrylcholinesterase