Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
24369840
DOI
10.1016/j.bmc.2013.12.016
PII: S0968-0896(13)01010-9
Knihovny.cz E-resources
- Keywords
- Cytotoxicity, Diethyl phosphate, In vitro antimicrobial activity, In vitro antimycobacterial activity, Salicylanilide,
- MeSH
- Anti-Bacterial Agents chemical synthesis chemistry pharmacology MeSH
- Antifungal Agents chemical synthesis chemistry pharmacology MeSH
- Bacteria drug effects MeSH
- Hep G2 Cells MeSH
- Fungi drug effects MeSH
- Humans MeSH
- Microbial Sensitivity Tests MeSH
- Molecular Structure MeSH
- Organophosphates chemical synthesis chemistry pharmacology MeSH
- Cell Proliferation drug effects MeSH
- Antineoplastic Agents chemical synthesis chemistry pharmacology MeSH
- Salicylanilides chemical synthesis chemistry pharmacology MeSH
- Drug Screening Assays, Antitumor MeSH
- Cell Survival drug effects MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Anti-Bacterial Agents MeSH
- Antifungal Agents MeSH
- Organophosphates MeSH
- Antineoplastic Agents MeSH
- Salicylanilides MeSH
A series of 27 salicylanilide diethyl phosphates was prepared as a part of our on-going search for new antimicrobial active drugs. All compounds exhibited in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium strains, with minimum inhibitory concentration (MIC) values of 0.5-62.5μmol/L. Selected salicylanilide diethyl phosphates also inhibit multidrug-resistant tuberculous strains at the concentration of 1μmol/L. Salicylanilide diethyl phosphates also exhibited mostly the activity against Gram-positive bacteria (MICs ≥1.95μmol/L), whereas their antifungal activity is significantly lower. The IC50 values for Hep G2 cells were within the range of 1.56-33.82μmol/L, but there is no direct correlation with MICs for mycobacteria.
References provided by Crossref.org
2-Hydroxy-N-phenylbenzamides and Their Esters Inhibit Acetylcholinesterase and Butyrylcholinesterase
Novel Cholinesterase Inhibitors Based on O-Aromatic N,N-Disubstituted Carbamates and Thiocarbamates
Salicylanilide diethyl phosphates as potential inhibitors of some mycobacterial enzymes
