Chromatography methods in investigation of lipophilicity of the biological active substances

Odović, Jadranka; Trbojević-Stanković, Jasna

doi:10.2298/hemind0901033o

Hem Ind

2009

DOI: 10.2298/hemind0901033o

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Chromatography methods in investigation of lipophilicity of the biological active substances

Jadranka Odović

Jasna Trbojević-Stanković

Abstract: This paper presents the review of the methods used in research of the biological active substances hydrophobicity, a very important property. The biological activity of some substances depends on their pharmacokinetics and pharmacodynamics. These processes depend on the molecule's capability to interact with two different media: aqueous (cells interior) and non-aqueous (cells membrane), or on the molecule lipophilicity. Today, great attention is given to investigation and systematic determination of drugs lipo… Show more

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2016

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“…The value logP is experimentally determined by the classical method of measuring distribution of organic compounds between the non-polar phase and water [14] using chromatographic [18], electrochemical [23] and other methods.…”

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The quantitative relationships of the partition coefficients calculated in the series of n-r-amine functional derivatives

et al. 2016

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Using on-line services and the ChemBioOffice2014 software package the values of the partition coefficients of some N-R-amine derivatives have been calculated. To identify the quantitative relationships and select the optimal algorithm of calculations the correlation and regression analysis of the values obtained has been conducted. Statistically significant values of correlation for the partition coefficients calculated have been determined. It has been shown that it is advisable to use the value AlogPs for further application.Lipophilicity is one of the criteria for assessing the similarity of synthetic substances and drugs, and it affects the biological activity of substances [9,13,14]. The partition coefficient of n-octanol-water (logP) characterizes physicochemical properties of substances in solutions and is used to simulate their behaviour in the body [3,14]. Distribution and redistribution of substances between lipophilic (fatty) and aqueous phases are part of biological processes, in particular transmembrane transport through lipid layers [11]. Hydrophobicity plays an important role in determining distribution of a substance in the body after absorption, its metabolic rate and elimination. The hydrophobic effect is essential for binding of drugs with their receptors [13].The ability to predict biological properties of compounds through their lipophilicity allows to optimize the search for new drugs and is often included in equations for calculations of the quantitative structure -activity relationships (QSAR) [16].The value logP is experimentally determined by the classical method of measuring distribution of organic compounds between the non-polar phase and water [14] using chromatographic [18], electrochemical [23] and other methods.However, experimental methods to determine logP are time-consuming and expensive, and the values obtained often differ due to the influence of many factors. Therefore, today a significant number of algorithms for theoretical calculations of values logP implemented using the appropriate software [5, 6, 8, 17,24, 25].The values of the partition coefficients of n-octanolwater experimentally obtained with the values theoretically calculated by different algorithms (AlogPs, IAlogP, ClogP, miLogP, logP KowWIN , xlogP3, etc.) were compared for 193 substances [19] and more than 96 000 compounds (including databases of Nykomed and Pfizer) [15]. In both studies the experimental data better correlate with the methods of AlogPs, xlogP3, logP KowWIN .Attempts to achieve proportionality of results of the theoretical calculation methods of prediction and the experimental determination of lipophilicity of organic compounds are still relevant in modern scientific studies [1, 16, 22].The aim of this work is to determine the mutual correlation of the values of the partition coefficients in the series of some functional derivatives of N-R-amines (1-21) calculated by different algorithms. Materials and MethodsTaking into account the data [15,19] we used the available free on-line methods xlog...

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The quantitative relationships of the partition coefficients calculated in the series of n-r-amine functional derivatives

et al. 2016

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Chromatography methods in investigation of lipophilicity of the biological active substances

Cited by 1 publication

References 27 publications

The quantitative relationships of the partition coefficients calculated in the series of n-r-amine functional derivatives

The quantitative relationships of the partition coefficients calculated in the series of n-r-amine functional derivatives

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