An antifungal agent is a drug that selectively eliminates fungal pathogens from a host with minimal toxicity to the host. Classes:
1. Polyene Antifungal Drugs: Amphotericin, nystatin, and pimaricin interact with sterols in the cell membrane (ergosterol in fungi, cholesterol in humans) to form channels through which small molecules leak from the inside of the fungal cell to the outside.
2. Azole Antifungal Drugs: Fluconazole, itraconazole, and ketoconazole inhibit cytochrome P450-dependent enzymes (particularly C14-demethylase) involved in the biosynthesis of ergosterol, which is required for fungal cell membrane structure and function.
3. Allylamine and Morpholine Antifungal Drugs: lylamines (naftifine, terbinafine) inhibit ergosterol biosynthesis at the level of squalene epoxidase. The morpholine drug, amorolfine, inhibits the same pathway at a later step.
4. Antimetabolite Antifungal Drugs: 5-Fluorocytosine acts as an inhibitor of both DNA and RNA synthesis via the intracytoplasmic conversion of 5-fluorocytosine to 5-fluorouracil.
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iKIX1 is a small-molecule inhibitor of the interaction of the C. glabrata Pdr1 activation domain with the C. glabrata Gal11A KIX domain with Ki of 18 uM; blocks Gal11/Med15 recruitment and inhibits Pdr1-dependent gene activation and re-sensitizes drug-resistant C. glabrata to azole antifungals in vitro and in animal models for disseminated and urinary tract C. glabrata infection; a novel therapeutic strategy in fungal infectious disease.
ML316(ML 316) is a specific antifungal agent that fungal-selectively inhibits the mitochondrial phosphate carrier Mir1, exhibits potent antifungal activity against the moderatelyazole-resistant C. albicans strain CaCi-2 with MIC of 0.05 ug/ml; kills drug-resistant Candida species at nanomolar concentrations; diminishes mitochondrial oxygen consumption, resulting in an unusual metabolic catastrophe marked by citrate accumulation and death in respiring yeast; reduces fungal burden and enhances azole activity in mouse model of azole-resistant oropharyngeal candidiasis.
SCY-078 (MK-3118;MK 3118;SCY 078) is a novel orally bioavailable fungal beta-1,3-D glucan synthetase inhibitor against Candida species C. glabrata (MIC 0.03 to 0.25 ug/ml), C. parapsilosis (MIC 0.06 to 0.25 ug/ml); shows actvity in an in vivo neutropenic murine model.
VT-1161(VT1161) is a potent, highly-selective, and oral fungal CYP51 inhibitor with Kd of ≤ 39 nM; demonstrates >2,000-fold selectivit over human CYP51, weakly inhibits human CYP2C9, CYP2C19, and CYP3A4; exhibits excellent potency against key yeast and dermatophyte strains.
Voriconazole (UK-109496;UK109496;UK 109496) is a triazole antifungal agent that acts as a 14α-demethylase inhibitor; used to treat and prevent invasive fungal infections including aspergillosis andcandidiasis and fungal infections caused by Scedosporium and Fusarium species.
Fosfluconazole is a water-soluble, phosphate prodrug of fluconazole, a triazole antifungal agent and 14-alpha demethylase inhibitor used in the treatment and prevention of superficial and systemic fungal infections.
Butenafine hydrochloride is a synthetic benzylamine antifungal that inhibits the synthesis of ergosterol by inhibiting squalene epoxidase; displays superior activity against Candida albicans than terbinafine and naftifine; demonstrates low MICs against Cryptococcus and Aspergillus.
Posaconazole hydrate (SCH-56592 hydrate) is a triazole antifungal agent that blocks the synthesis of ergosterol by inhibiting of the enzyme lanosterol 14α-demethylase and accumulation of methylated sterol precursors, more potent at inhibiting 14α-demethylase than itraconazole.
A polyene antifungal antibiotic that works by disrupting the cell membrane of the fungal cells.
Posaconazole (SCH-56592) is a triazole antifungal agent that blocks the synthesis of ergosterol by inhibiting of the enzyme lanosterol 14α-demethylase and accumulation of methylated sterol precursors, more potent at inhibiting 14α-demethylase than itraconazole.
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