Abstract
SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF BENZIMIDAZOLYL-ARYLPROPENONE SCAFFOLDS AS PROMISING INHIBITORS OF AZOLE-RESISTANT CANDIDA STRAINS

Coulibaly Songuigama, N'guessan D. U. Jean-Paul, Ouattara Mahama*, Kone W. Mamidou and Sissouma Drissa

ABSTRACT

In the general context of the emergence of strains resistant to currently available antifungal drugs, we herein report the synthesis and the antifungal activities of some benzimidazoles-arylpropenones against three Azole-resistant Candida strains. These compounds were afforded by a Claisen-Schimdt type condensation reaction between 2-acetylbenzimidazole and the aromatic aldehydes. The chemical structures of the compounds were determined by the usual spectroscopic methods (1H and 13C NMR, MS). The in vitro antifungal activities were assessed on clinical strains of Candida albicans, C. glabrata and C. tropicalis by the microplate dilution method. The results showed that of the 10 compounds tested, 7 possessed antifungal activities unlike the reference drugs (Fluconazole and Ketoconazole) which showed no activity at our limit threshold of 10 μg. Furthermore, two compounds are particularly illustrated by their anti-Candida effectiveness on all three strains with MIC between 1.25 and 5μg / mL.

Keywords: Benzimidazole. Arylpropenone. Azoles. Candida albicans. Candida glabrata. Candida tropicalis.


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