Polyene macrolides have historically been the first antibiotics used in antifungal therapy. The discovery of nystatin and amphotericin in 1950s provided new opportunities for treatment of various fungal infections. Later, more than 200 other polyene macrolides with antifungal activity have been discovered, although only amphotericin B and nystatin have found substantial use , nystatin, candicidin, pimaricin, methyl partricin and trichomycin are currently being used in human therapy. In general, the polyene macrolides are rather toxic, and may cause such serious side-effects as renal tubular damage and thrombophlebitis, especially upon intravenous administration. Despite of that, broad spectrum of activity and low frequency of appearance of resistant pathogens make polyene antibiotics, like amphotericin B, the drug of choice when dealing with life-threatening systemic fungal infections. Polyene antibiotics display a unique mode of action by making the fungal cell membranes permeable to ions and other small molecules via polyene-ergosterol interactions.