Relationship of antimicrobial activity and chemical structure of the arylaliphatic aminoalcohol derivatives
Journal Title: Фармацевтичний журнал - Year 2015, Vol 5, Issue 5
Abstract
Arylaliphatic aminoalcohols appeared to be the new promising class of compounds for the development of antibacterial and antifungal agents. The aim of the presented study was to analyze the «chemical structure-antimicrobial activity» relationship for further activity-directed synthesis of compounds of this class. The antimicrobial activity of the compounds was investigated by serial broth dilution method. Primary analysis of the effect of substituents’ structure on the ability of the derivatives to inhibit the growth of test-microorganisms was carried out by empirical method. Molecular structural characteristics of arylaliphatic aminoalcohols (surface area, volume, partition coefficient logP and dipole moment) were calculated by means of «Hyperchem 8.0.8» software. Relationship between the antimicrobial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and molecular characteristics was investigated by correlation analysis using the Spearman test. Statistical processing was performed by «StatSoft Statistica 6.0», the data obtained were evaluated using Chaddock scale. The data obtained suggest, that the presence of both antibacterial and antifungal activity in arylaliphatic aminoalcohols depends on the amino group structure and composition of aryl(alkyl)oxy-radical (4-(1,1,3,3-tetramethylbutyl)phenyl, 1-adamantyl, 4-(1-adamantyl)phenyl, 4-phenyl-phenyl or 2,4-ditretbutyl phenyl). The correlation analysis revealed an inverse relationship between the antimicrobial action and surface area, volume, and lipophilicity of compounds. The tightest correlation was found between these parameters and antistaphylococcal activity. Our results indicate the promises of the synthesis, directed to the reducing of the molecule size and lipophilicity of tetramethylbutylphenyl aminoalcohols, for further development of broad-spectrum antimicrobial agents.
Authors and Affiliations
M. L. Dronova, Z. S. Suvorova, Yu. V. Korotkyi
Keywords
Related Articles
- EP ID EP586649
- DOI -
- Views 44
- Downloads 0
Research of acute toxicity of the drug HEXIA
Diseases of the genitourinary system caused by pathogenic and potentially pathogenic microorganisms, which result into disbiosis of urinary organs, remain an urgent problem of dermatovenereology, gynecology and urology,...
Analysis of the pneumonia morbidity in children in order to optimize pharmaceutical aid
To analyze the health of the child population used statistical incidence, disease prevalence, their gender features and age characteristics, mortality. According to WHO, among the major causes of child mortality, the sh...
Determination of esters and amides of aminobenzoic acid in the composition of finished dosage forms with acidic monoazo-dye tropaeolin O
Esters of aminobenzoic acid are widely used in medical practice as effective painkillers of local action, and its amide as is an antiarhythmic drug. The peculiarity of these drugs, in terms of analytical control, is a lo...
Investigation of chemical composition of aster purple loosestrife (Aster salignus Willd)
In modern medicine is paid much attention for the search of new sources of natural bioactive compounds. The genus aster (Aster L.) aster family (Asteraceae) includes more than 500 species of herbaceous perennials, widesp...
Conceptual foundations of pharmacoeconomic analysis of prevention technologies of chronic viral infections
The introduction of various technologies for the prevention of chronic viral infections into practice requires well-founded evidence of their effectiveness, which can be obtained using pharmacoeconomic methods and models...