Candida is a genus of yeasts and is the most common cause of fungal infections worldwide. However, only a few antifungal drugs are currently available for the treatment of Candida infections. In the last decade, terpenophenols have attracted much attention because they often possess a variety of biological activities. In the search for new antifungals, eight carveoylphenols were synthesized and characterized by spectroscopic analysis. By using the broth microdilution assay, the compounds were evaluated for antifungal activities in vitro against four human pathogenic yeast, and structure–activity relationships (SAR) were derived. Noteworthy, in this preliminary study, compounds 5 and 6, have shown a significant reduction in the growth of all Candida strains tested. Starting from these preliminary results, we have designed the second generation of analogous in this class, and further studies are in progress in our laboratories.