Candidiasis is one of the most widespread fungal infections globally. The efficacy of antifungal chemotherapy has become a public health concern due to the emergence and proliferation of drug-resistant Candida strains. It is within this context that we proposed to design, synthesize, and evaluate the antifungal activities of a new series of 2-styrylbenzimidazoles against a clinical strain of Candida glabrata. The objective of this work was to identify a potential antifungal lead compound to initiate its medicinal chemistry development. The 2-styrylbenzimidazoles used were conceptualized using medicinal chemistry techniques involving the hybridization of chemical entities with potential antifungal properties. The antifungal activities of the compounds were expressed as Minimum Inhibitory Concentrations (MICs), determined in vitro against a clinical strain of C. glabrata using the microplate dilution technique. All 10 evaluated compounds exhibited antifungal activity against the clinical strain of Candida glabrata. Furthermore, the derivative chlorinated at the 2-position of the benzene ring stood out for its particular efficacy against Candida, with an MIC of 12.26 μM. In conclusion, the derivative chlorinated at position 2 can be selected as the “hit molecule” from which further pharmacomodulations can be undertaken to obtain a drug candidate for the medicinal chemistry development of a new class of antifungals based on the 2-styrylbenzimidazole profile.
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