Chemical Industry and Chemical Engineering Quarterly 2011 Volume 17, Issue 1, Pages: 9-15
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Lipophilicity and antifungal activity of some 2-substituted benzimidazole derivatives

Podunavac-Kuzmanović Sanja O., Cvetković Dragoljub D.

In the present paper, the antifungal activity of some 2-methyl and 2- aminobenzimidazole derivatives was evaluated against yeast Saccharomyces cerevisiae. The tested compounds displayed in vitro antifungal activity and minimum inhibitory concentration (MIC) was determined for all compounds. The partition coefficients of the studied compounds were measured by the shake flask method (logP) and by theoretical calculation (ClogP). The logP values were compared and the relationships between the logP values and antifungal activities were investigated. The mathematical models have been developed as a calibration models for predicting the antifungal activity of this class of compounds. The quality of models was validated by leave one out (LOO) technique as well as by the calculation of statistical parameters for the established models. The results of the present study may be useful for the designing of new more potent benzimidazole derivatives against yeast Saccharomyces cerevisiae.

Keywords: Benzimidazole, antifungal activity, lipophilicity, quantitative structure activity relationship, Saccharomyces cerevisiae

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