Promising new compounds have recently been identified in an effort to supplement the relatively sparse portfolio of antifungal drugs. Many of these compounds have defined mechanisms of action against fungal cells and have, in some cases, aided the identification of new selective targets in fungi. For most of these compounds, however, factors such as a narrow spectrum of activity, susceptibility to efflux pumps, protein binding, serum inactivation and poor pharmaceutical properties prevent their use in the clinic. Even so, these compounds are novel substrates for synthetic modifications that could lead to the discovery of future antifungal drugs.