Antifungals

Antifungals (also known as antimycotics) are a pharmacologically diverse group of compounds used to treat mycoses (fungal infections) in humans and animals. They may also be used in cell culture to prevent contamination. Most antimycotic products act by interfering with the integrity of the fungal cell membrane or cell wall.

Products
Background
Literature (1)
Cat. No. Product Name / Activity
6930 Amphotericin B
Antifungal; binds ergosterol in fungal cell membranes
6384 Ciclopirox
Antifungal; pan-histone demethylase inhibitor
4096 Clotrimazole
Imidazole antimycotic and cytochrome P450 inhibitor
0970 Cycloheximide
Antifungal antibiotic; preferentially inhibits protein synthesis in eukaryotes
6250 Filipin III
Polyene antibiotic; binds sterols in fungal membranes.
3764 Fluconazole
Triazole antifungal agent
5981 Itraconazole
Azole antifungal; also SMO antagonist
1987 Leptomycin B
Antifungal antibiotic; inhibits nuclear export of proteins
3016 Miconazole nitrate
Azole antifungal agent
3197 Polygodial
Exhibits antifungal activity via inhibition of mitochondrial ATPase; also TRPA1 channel activator
1589 Radicicol
Antifungal antibiotic
6484 Terbinafine hydrochloride
Antifungal; inhibits fungal sterol biosynthesis
5270 Toyocamycin
Antifungal antibiotic; adenosine analog
3760 Voriconazole
Triazole antifungal agent

Antimycotic Mechanism of Action

The majority of antimycotic compounds, including the azole antifungals such as Fluconazole, the polyene antibiotics such as Amphotericin B, and the allylamine, Terbinafine, exert their effects via disruption of the fungal cell membrane. Azoles are inhibitors of sterol 14α-demethylase, a fungal cytochrome P450 (CYP)-dependent enzyme, which results in depletion of cell membrane ergosterol and impaired membrane fluidity, leading to accumulation of toxic 14α-methylated sterols and eventual fungal cell death. Terbinafine also inhibits ergosterol synthesis, but by a different route, the inhibition of squalene monooxygenase. Amphotericin B, on the other hand directly binds to ergosterol, forming complexes that intercalate the cell membrane and form pores.

Ciclopirox, another antimycotic, is a non-selective histone demethylase inhibitor. Among other types of antimycotics, the echinocandins act by disrupting cell wall synthesis, while compounds such as griseofulvin and flucytosine, affect mitosis.

Mycosis

Mycoses, or fungal infections, can be classified according to the site and extent of infection, as local (superficial, cutaneous or subcutaneous) or systemic, and range from common benign infections, such as athlete's foot (tinea pedis), to the life threatening, such as Aspergillosis or cryptococcal meningitis. Mycoses can occur as a result of inhalation of fungal spores, cutaneous exposure or percutaneous inoculation. In addition, mycoses can result from an endogenous process such as reactivation of an infection or from abnormal activation of normally harmless flora. An example of this is tinea versicolor, which is caused by a normally benign fungus, Malassezia furfur, that lives on human skin; heat and humidity or a compromised immune system can lead to this infection causing skin symptoms consisting of skin discoloration and flaking, usually on the trunk, abdomen and neck. Individuals with compromised immune systems, such cancer patients undergoing chemotherapy, patients with HIV/AIDS, or those receiving steroids are at greatest risk of developing serious, opportunistic, invasive fungal infections.

Literature for Antifungals

Tocris offers the following scientific literature for Antifungals to showcase our products. We invite you to request* or download your copy today!

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Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

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