Abstract
Six novel imidazoline derivatives were synthesized and tested in antifungal assays. One of the compounds, N-cyclohexyl-2-imino-3-(4-nitrophenyl)imidazolidine-1-carboxamide showed moderate activity against several clinical strains of Candida albicans. Its structure was solved by X-ray crystallography and its mode of action was deduced using molecular modelling. It was found to be similar to that of fluconazole. The potential for further optimization including SAR of the compound is briefly discussed.
Highlights
Candida spp. encompasses a class of fungi that includes over 150 species
The compounds presented in this manuscript were synthesized as outlined in Scheme 1
Antifungal activity against clinical isolates of C. albicans was within MIC values ranged from 0.98 to ≥1000 mg/L (Table 2)
Summary
Candida spp. encompasses a class of fungi that includes over 150 species. It exists harmlessly in the body and is a component of the human mycobiome. Invasive fungal infections (IFIs) are the most serious type in which brain, heart, blood or other important parts of the body are infected [7,8]. These present the biggest challenge especially in the light of increased occurrence over the past decades and the urgent need for more effective drugs [9]. During the course of another investigation [13] we studied novel urea derivatives with antiproliferative properties Having accounted for their cytotoxicity and the need for protection of the natural microbiological flora we deemed it necessary to check how they influence survival of different microorganisms. We were interested in assessing antifungal activity because of the similarity to imidazole drugs currently in clinical use
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