Abstract

The reversed-phase high-performance liquid chromatographic (HPLC) method of hydrophobicity evaluation based on polybutadiene-coated alumina columns was applied in quantitative structure-activity relationship (QSAR) studies of a group of pharmacologically active azole derivatives. The solutes (weak organic bases) were chromatographed at pH 7.30 and 11.5. The HPLC data obtained under alkaline conditions correlated well with hydrophobicity parameter calculated for non-ionized forms of the compounds. The same chromatographic data were demonstrated to provide the most significant information on the biological activity of the compounds under study. The polymer-coated alumina stationary phases developed by Schomburg and co-workers, which can be used over a wide range of eluent pH values and which show no tendency to undergo the specific interactions with solutes typical of silica-based materials, offer unique advantages from the point of view of QSAR applications.

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