<abstract xmlns="http://www.w3.org/1999/xhtml">The aim of this paper is the study of physico-chemical properties of the chosen compounds, derivatives of 2-hydroxy-3-[2-(4-methoxyphenyl)
ethylamino]propyl-4-[(alkoxycarbonyl)amino]benzoates and 2-hydroxy-3-[2-(2-methoxyphenyl)ethylamino]propyl-4-[(alkoxycarbonyl)
amino]benzoates with potential ultra-short beta-adrenolytic activity. The studied compounds are different in the
position of the substituent on the benzene ring in the side chain as well as in the aromatic ring in position 4 with alkyl- (methylto
butyl-) carbamate. The physico-chemical characteristics, for example, lipophilicity, surface activity, adsorbability, acidobasic
properties etc., are very important for the explanation of the relationship between structure and biological activity of the drug.
These parameters serve as the base of quantitative structure-activity study. The goal of this work is to establish the spectral characteristics
of studied compounds in UV-area, pKa values, the parameters of lipophilicity (the values of Rf and RM from thin layer
chromatography, retention time t´R and capacity factor k´ from liquid chromatography and experimental partition coefficients
log P´ values), surface tension, critical micelle concentrations, the adsorbability of compounds expressed by percent of adsorbed
compound on active charcoal β% as well as by Freundlich adsorption isotherms. The obtained values are correlated with the
parameters characterising the size of molecule, for example, the number of carbon atoms on carbamate functional group.</abstract>

The aim of this paper is the study of physico-chemical properties of the chosen compounds, derivatives of 2-hydroxy-3-[2-(4-methoxyphenyl)
ethylamino]propyl-4-[(alkoxycarbonyl)amino]benzoates and 2-hydroxy-3-[2-(2-methoxyphenyl)ethylamino]propyl-4-[(alkoxycarbonyl)
amino]benzoates with potential ultra-short beta-adrenolytic activity. The studied compounds are different in the
position of the substituent on the benzene ring in the side chain as well as in the aromatic ring in position 4 with alkyl- (methylto
butyl-) carbamate. The physico-chemical characteristics, for example, lipophilicity, surface activity, adsorbability, acidobasic
properties etc., are very important for the explanation of the relationship between structure and biological activity of the drug.
These parameters serve as the base of quantitative structure-activity study. The goal of this work is to establish the spectral characteristics
of studied compounds in UV-area, pKa values, the parameters of lipophilicity (the values of Rf and RM from thin layer
chromatography, retention time t´R and capacity factor k´ from liquid chromatography and experimental partition coefficients
log P´ values), surface tension, critical micelle concentrations, the adsorbability of compounds expressed by percent of adsorbed
compound on active charcoal β% as well as by Freundlich adsorption isotherms. The obtained values are correlated with the
parameters characterising the size of molecule, for example, the number of carbon atoms on carbamate functional group.

Study of physico-chemical properties of potential beta-adrenolytics

Comenius University in Bratislava, Faculty of Pharmacy, Department
of Pharmaceutical Chemistry, Slovak republic

University of Veterinary and Pharmaceutical Sciences Brno, Faculty
of Pharmacy, Department of Chemical Drugs, Czech republic

European Pharmaceutical Journal

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

{"article-title":"Study of physico-chemical properties of potential beta-adrenolytics"}

The aim of this paper is the study of physico-chemical properties of the chosen compounds, derivatives of...

Study of physico-chemical properties of potential beta-adrenolytics

Publié en ligne: 30 déc. 2014

Pages: 49 - 54

DOI: https://doi.org/10.2478/afpuc-2014-0014

Mots clés
ultra-short-acting beta-blockers, lipophilicity, adsorbability, critical micelle concentration

© Acta Facultatis Pharmaceuticae Universitatis Comenianae

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Study of physico-chemical properties of potential beta-adrenolytics

Publié en ligne: 30 déc. 2014

Pages: 49 - 54

DOI: https://doi.org/10.2478/afpuc-2014-0014

Mots clésultra-short-acting beta-blockers, lipophilicity, adsorbability, critical micelle concentration

© Acta Facultatis Pharmaceuticae Universitatis Comenianae

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Mots clés
ultra-short-acting beta-blockers, lipophilicity, adsorbability, critical micelle concentration