Evaluating the Fungistatic and Fungicidal Activities of Bianthrones as Synthetic Intermediates to Novel Hypericin Analogues.

Abstract

There is increasing demand for new and improved antifungal agents due to an increase in fungal infections and diseases in patients being resistant to previous antifungals. The focus of this research is on the synthesis of anthraquinone, anthrone, bianthrone and hypericin type derivatives and the effect they have on the growth of the yeast species Schizosaccharomyces pombe, Lipomyces starkeyi andSaccharomyces cerevisiae. It is hoped that a new antifungal agent could be identified to combat the threat of these resistant fungi in order to treat patients who have compromised immune systems due to HIV/AIDS, cancer treatments or in the case of organ transplant patients due to the presence of immune suppressants. The research approach adopted in this study includes the synthesis of anthraquinone, anthrone and bianthrones as hypericin derivatives and their effect on yeast by a growth inhibition assay. The findings of this research are that these derivatives give interesting results in the yeast growth inhibition assays with a few of the compounds synthesised being fungicidal in their activity and many of the compounds showing low inhibitory concentrations. The main conclusions drawn from this research are that the anthraquinone, anthrone, bianthrone and hypericin type derivative compounds, especially the amine derivatives of anthraquinone, show promise in the area of antifungal agents. The recommendations are that more derivatives are synthesised and the growth inhibition assay is repeated, testing for resorufin fluorescence inhibition, which gives greater sensitivity.