Broad screening revealed compound 1a to be a novel anti-fungal agent with high specificity towards dermatophytes. The anti-fungal structure–activity relationship of this novel class of 5, 6-dihydro-4H-pyrrolo [1, 2-a][1, 4] benzodiazepines is described together with its mode of action that appeared to be the inhibition of squalene epoxidase. Preliminary in vivo results of the most active compounds are also reported.
