Antifúngicos

ATPase-IN-5 (Compound 11) is an antifungal Pma1p (H+ -ATPase) inhibitor (IC50 = 12.7 μM) that inhibits the growth of Candida albicans and Saccharomyces cerevisiae.

D75-4590, a β-1,6-Glucan synthetase inhibitor, combats fungal infections by targeting cell walls.

Caspofungin is an echinocandin that belongs to the class of antifungal agents. It is used to treat Aspergillus and Candida infections. It works by inhibiting the synthesis of beta-(1,3)-D-glucan, an essential component of the cell wall of Aspergillus species and Candida species.

Amphotericin A is a polyene macrolide antibiotic, which is derived primarily from the soil bacterium *Streptomyces nodosus*. This compound functions by binding to ergosterol, an essential component of fungal cell membranes. This binding creates pores in the membrane, increasing its permeability and ultimately leading to cell death. Unlike its more widely used counterpart Amphotericin B, Amphotericin A is less frequently utilized but is critical in the study and understanding of antifungal activity.

Delafloxacin is a fluoroquinolone antibiotic with action on bacterial DNA gyrase and topoisomerase IV and is used for treating acute bacterial skin and skin structure infections.

Voriconazole is a synthetic, lipophilic molecule that is used in the treatment of fungal infections. Voriconazole binds to ergosterol which is the major sterol in the cell wall of fungi and inhibits its synthesis, leading to cell death. This drug binds to the enzyme 14α-demethylase allowing the conversion of lanosterol into ergosterol. As a result, this binding leads to the inhibition of ergosterol synthesis, as well as other sterols that are necessary for fungal growth (e.g., squalene).

Micafungin, as one of three echinocandina, has been proven to be a successful antifungal therapeutic in treating general Candida fungus infections. The treatment of immunocompromised patients is particularly important as Candida infections cause high mortality rates in patients in intensive care units, receiving chemotherapy, or stem cell transplants. This product acts as an anti-fungal by inhibiting the 1,3-beta-D-glucan synthase enzyme. As a result the production of 1,3-beta-D-glucan, which is crucial to the fungal cell wall, is hindered. Thus, the fungal cell wall loses integrity allowing for osmotic instability and cell lysis to occur.

Posaconazole is an antifungal agent that inhibits the 14-alpha demethylase enzyme which is responsible for the synthesis of the fungal cell wall component, ergosterol. This demethylase enzyme synthesizes ergosterol through converting lanosterol to ergosterol. Therefore Posaconazole prevents the formation of fungal cell walls with the appropriate membrane permeability thus leading to fungal cell lysis. Posaconazole can be used as an antifungal drug to treat opportunistic fungal infections in immunocompromised individuals such as HIV patients. Moreover it is shown to inflict its inhibitory activity against common pathogenic fungus such as Candida and Aspergillus species but also Mucorales and some Fusarium species, which are less common.

Ciclopirox is a broad-spectrum antifungal agent that is used to treat onychomycosis of fingernails and toenails in immunocomprised patients. Ciclopirox has been shown to work by binding to polyvalent metal cations such Al3+ and Fe3+. These cations interfere with cellular processes including mitochondrial electron transport and energy synthesis by inhibiting numerous enzymes, including cytochromes. Additionally, the plasma membrane of fungi appears to be altered by ciclopirox as well, leading to the disorder of internal structures.

Amorolfine is an antifungal drug that inhibits fungal enzymes (D14 reductase and D7-D8 isomerase). Its inhibition has an affect on fungal sterol synthesis pathways, and it depletes ergosterol. This drug can be used as a treatment for inflammatory lesions such as Tinea corporis, Tinea pedis, and Tinea cruris due to its ability to penetrate the skin barrier with ease.

Atovaquone is an antimicrobial drug that is used for the treatment of Pneumocystis jirovecii pneumonia. This drug is an analog of ubiquinone and has good in vitro activity against Toxoplasma gondii.

Terconazole is an azole antifungal agent with action on fungal cell membranes by inhibiting ergosterol biosynthesis and is used for treating vaginal yeast infections.

Abafungin is an antifungal agent and is used for treating fungal infections.

21-Norrapamycin is a macrocyclic lactone antibiotic, which is derived from the bacterium Streptomyces hygroscopicus. Its chemical structure is closely related to that of rapamycin, a well-known immunosuppressant. The mode of action of 21-Norrapamycin involves the inhibition of the mechanistic target of rapamycin (mTOR) signaling pathway. By binding to the FK506-binding protein 12 (FKBP12), it forms a complex that then inhibits mTOR, a crucial regulator of cell growth, proliferation, and survival.

Malformin C is a cyclic pentapeptide, which is a secondary metabolite derived from certain strains of the fungus Aspergillus. Its mode of action involves disrupting cellular processes by interfering with cell division. Specifically, it is thought to affect mitotic spindle formation, leading to abnormal cell cycle progression.