Antifungal agents: past, present and future

A. Zarei Mahmoudabadi

Author address: 



The first efforts to find antifungals agents have been started from nineteenth century. Lime sulfur and boiled lime sulfur were respectively used for the treatment of powdery mildew of apple and grape, during 1803-1833. Fungicidal property of formaldehyde was recognized in 1888 and formalin used as anti-wheat smut in 1897. Griseofulvin was isolated from Penicillium griseofulvum (1939) and introduced as the first oral antifungal for the treatment of dermatophytoses in 1958. Although nystatin was the first clinically used antifungal, amphotericine B was more effective antifungal agent against deep mycosis during last five decades. Toxicity of amphotericin B limit its use, however it is still first choice for systemic mycoses. New class of antifungal drugs (Azoles) introduced with licensing clotrimazole in 1969. During last four decades, several azoles, such as miconazole, fluconazole, ketoconazole and itraconazole presented as orally/topically for the treatment of cutaneous and/or systemic mycosis. Terbinafine was also described as more effective antifungal drug against several fungi, yeasts, saprophytic fungi, dermatophytes and dimorphic fungi during two decades. Important progress has been achieved in antifungal chemotherapy in recent years. FDA approved the new systemic antifungal echinocandins (micafungin, and anidulafungin) and posaconazole in 2005 and 2006. Both micafungin and anidulafungin inhibit the synthesis of [beta]- D-glucan in fungal cell walls. Posaconazole is a triazole antifungal that inhibits cytochrome P450 14a-demethylase (P45014DM). Drug is effectively used to the treat zygomycosis due to Mucor. Bafilomycin K is a new antifungal macrolide that isolated from Streptomyces flavotricini (Y12-26) . Herbal and alternative medicines are popular in the general population worldwide. A great number of modern drugs are still derived from herbs sources. The antifungal activity of several herbs, Allium sativum, Zingiber officinalis, Glycyrrhiza glabra, Aloe Vera and Mentha piperita was investigated in vitro system in several countries. However few herbs are used as effective antifungal in clinic. Future trends for the development of antifungal agents with fungicidal activity, wider spectra, nontoxic and better distribution from natural sources are proposed. In addition, the combination of antifungal chemotherapy with immunotherapy is a new protocol for fungal infections in immunocompromised patients.

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Full conference title: 

Iranian Congress on Medical Mycology
    • ICMM 2011