LIPOPHILICITY AND ANTIFUNGAL ACTIVITY OF SOME 2-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES

Abstract

In the present paper, the antifungal activity of some 2-methyl and 2-amino-benzimidazole derivatives was evaluated against yeast Saccharomyces cere¬visiae. The tested compounds displayed in vitro antifungal activity and mini¬mum inhibitory concentration (MIC) was determined for all compounds. The partition coefficients of the studied compounds were measured by the shake flask method (log P) and by theoretical calculation (Clog P). The log P values were compared and the relationships between the logP values and antifungal activities were investigated. The mathematical models have been developed as calibration models for predicting the antifungal activity of this class of com¬pounds. The quality of models was validated by the leave-one-out (LOO) technique as well as by the calculation of statistical parameters for the esta¬blished models. The results of the present study may be useful for the de¬signing of new more potent benzimidazole derivatives against yeast Sac-charo¬myces cerevisiae.

Keywords

• benzimidazole
• antifungal activity
• lipophilicity
• quantitative structure-activity relationship
• Saccharomyces cerevisiae