Quantitative relationships between structure and antimicrobial activity of new "soft" bisquaternary ammonium salts
Language English Country United States Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
7995599
DOI
10.1007/bf02814644
Knihovny.cz E-resources
- MeSH
- Anti-Bacterial Agents MeSH
- Antifungal Agents chemical synthesis pharmacology MeSH
- Anti-Infective Agents chemical synthesis pharmacology MeSH
- Candida albicans drug effects MeSH
- Escherichia coli drug effects MeSH
- Quaternary Ammonium Compounds pharmacology MeSH
- Microbial Sensitivity Tests MeSH
- Surface-Active Agents pharmacology MeSH
- Staphylococcus aureus drug effects 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
- Anti-Infective Agents MeSH
- Quaternary Ammonium Compounds MeSH
- Surface-Active Agents MeSH
New surface-active bisquaternary ammonium salts derived from bis-(2-dimethylaminoethyl) ester of glutaric acid are highly effective against representatives of Gram-positive, Gram-negative bacteria and yeasts. Relationships between structure, lipophilicity and antimicrobial effectiveness were demonstrated by quantitative structure-activity methodology. The non-linear dependence of biological activity on the structure as well as lipophilicity (expressed as critical micelle concentration-CMC) was shown using Kubinyi's bilinear model. The most effective compounds were those with the alkyl chain of 11-12 carbon atoms and with the CMC values around 0.7-1.0 mmol/L. These derivatives possessed higher antimicrobial activity particularly to Gram-negative bacteria.
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