Invasive fungal infections are increasing worldwide due to an expanding number of immunocompromised patients as well as an increase in drug resistant fungi. While fungal resistance has increased, this resistance has not been accompanied by the development of new antifungals. Fluconazole, part of the azole class of antifungals, has been shown to be less effective with the increase in resistant fungal pathogens. Therefore, the development of novel azole antifungal compounds is of urgent need. The goal of this research is to synthesize novel triazole containing small molecules with potent antifungal activity. The scaffold of the synthesized compounds contains a triazole moiety and are synthesized via a copper-catalyzed 1,3-dipolar cycloaddition (click chemistry) between the appropriate alkyne and azide intermediates. The use of the click reaction was intentional as it is a reaction that is high yielding, wide in scope, regiospecific, simple to perform, and conducted in aqueous conditions usually at room temperature. The minimum inhibitory concentrations of these compounds will be determined using standard broth microdilution assays against fungi associated with life-threatening invasive fungal infections. The objective of this research is to develop and optimize lead compounds with potent <i>in vitro </i>antifungal activity. The application of an iterative structure-activity relationship (SAR)-driven approach, where each set of biological data guides the synthesis of next generation analogues, will provide new compounds with increased efficacy.

Synthesis of novel triazole containing small molecules as potential antifungal compounds

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