ABSTRACT
Due to the distinct potential applications of squalene epoxidase inhibitors – treatment of fungal infections by selective blocking of ergosterol biosynthesis in fungi, or lowering of cholesterol levels by inhibition of human sterol biosynthesis — differential biological profiles of the drugs and, hence, different test systems were required for the respective indication. Due to the existence of highly active and selective fungal squalene epoxidase inhibitors (the allylamine, the homopropargylamine, the benzylamine, and the thiocarbamate antimycotics), squalene analogues have been of no importance as inhibitors of the fungal enzyme. Allylamine derivatives constitute the most important class of squalene epoxidase inhibitors. A first group of compounds is highly selective for the fungal enzyme and used safely and successfully in the topical and systemic therapy of mycoses. A second group selectively inhibits mammalian squalene epoxidase, and appears to have a promising potential for the treatment of hypercholesterolemia.
