N. Ryder
Dec 1, 1988
Citations
0
Influential Citations
45
Citations
Journal
Annals of the New York Academy of Sciences
Abstract
The allylamines are a recently developed class of synthetic antifungal agents currently represented by naftifine, which is a topical antimycotic, and terbinafine, which is in advanced clinical trials for both topical and oral application. These compounds are effective against a wide range of pathogenic fungi and have exceptionally high activity against dermatophytes.14 A large number of related compounds have been synthesized and tested for antifungal activity.’.6 Naftifine7 and terbinafine’ and many related structures have been found to act by inhibiting fungal ergosterol biosynthesis specifically at the point of squalene epoxidation (FIG. 1). The allylamines are thus functionally as well as chemically distinct from the other major classes of antifungal agents. Extensive studies of the biochemical properties of the allylamines have been carried out in order to provide a physiological and enzymatic basis for their biological and clinical activity. The characteristics of the latter include the high efficacy against dermatophytes, the primary fungicidal action against many fungi, and the excellent tolerance in clinical use. This report summarizes our current knowledge of the biochemistry of the allylamines in both fungal and mammalian systems and of how this is translated into biological activity.