Synthesis and Evaluation of Functionalized Imidazole and Triazoles as Novel Anti-fungal Agents

Abstract

Fungal species are highly prevalent in our environment. Some are relatively harmless but there are others that are pathogenic. A problem arises when dermatophytes enter into the blood system. Commonly associated with immunocompromised patients, fungemia is when a fungal species enters the blood stream. Currently there are many treatments but there is a growing fear of resistance to these drugs and a need for novel therapeutics. The Baylis-Hillman reaction is a flexible template in which an aldehyde and various acrylates form a highly functionalized Baylis-Hillman derivative. In this paper, a small library of Baylis-Hillman reaction-derived imidazole and triazoles are synthesized and characterized. Furthermore, their anti-fungal activities are evaluated against <italic>Candida albicans</italic> and <italic>Cryptococcus neoformans</italic>. It was found that some of the derivatives showed moderate to good activity against <italic>Candida albicans</italic> (MIC 213-46.5 µg/ml) and <italic>Cryptococcus neoformans</italic> (MIC 5.50-1.68 µg/ml).