Mohamed I. Attia, Maha S. Almutairi, Soraya W. Ghoneim, Azza S. Zakaria and Hazem A. Ghabbour

Department of Pharmaceutical Chemistry; Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

Abstract:

A significant increase in fungal infections has been observed over the past two decades. Many reports of invasive topical and systemic infections caused by the opportunistic pathogen Candida species are always associated with the use of broad-spectrum antibiotics, immunosuppressive agents, anticancer and anti-AIDS drugs. The synthesis and anti-Candida activity of ({[1-arylpropylidene]amino}oxy)-3-(1H-imidazol-1-yl)-arylmethanones 5a-h are reported. The stereochemistry of the title compounds 5a-h was proved via single crystal x-ray crystallography. Among the newly developed bioactive chemical entities, compound 5b emerged as the most potent congener in the whole synthesized compounds. It displays minimum inhibitory concentration (MIC) of 1.9 μg/mL against Candida albicans being four-fold and 60-fold more potent than the clinically used antifungal drugs Miconazole and Voriconazole, respectively.

Keywords: Synthesis, Anti-Candida, Single Crystal X-ray and imidazoles.