fluconazole

Fluconazole (UK-49858) is a triazole antifungal agent used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS.

Fluconazole (hydrate) is a triazole antifungal agent used for oral treatment and prevention of both superficial and systemic fungal infections, including but not limited to balanitis, various Candida infections, Cryptococcus infections, dermatomycosis, and fungal infections of the respiratory and urinary tracts. As the hydrate salt form of fluconazole, it exhibits antifungal activity by inhibiting the growth and development of pathogenic fungi, such as Candida species, at minimal inhibitory concentrations often exceeding 100 mg l. Notably, it disrupts the branching and hyphal formation in C. albicans at concentrations as low as 0.3 mg l, indicating its potency compared to other antifungals like miconazole and ketoconazole which are effective at 100-fold lower concentrations. Clinical studies have not shown a significant increase in the risk of most birth defects with oral fluconazole, although there may be an associated risk of tetralogy of Fallot. Its efficacy against Cryptococcus gattii in koalas suggests it may be ineffective as a sole therapeutic agent at a dosage of 10 mg kg orally every 12 h. Toxicity symptoms from overdose can include hallucinations and paranoid behavior.

Fluconazole (mesylate) is a triazole antifungal drug used for the treatment and prevention of both superficial and systemic fungal infections.

Fluconazole-d4 is a deuterated compound of Fluconazole. Fluconazole has a CAS number of 86386-73-4. Triazole antifungal agent that is used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS.

Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM). Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent.

Fosfluconazole is water-soluble phosphate prodrug of fluconazole. Fluconazole is an antifungal drug.

Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC50s of 8.092 and 45.320 μM for yeast and human. Inz-1 reverses Fluconazole or other triazole antifungals' resistance in the pathogenic fungus Candida albicans.

Terconazole (Terazol 7) is a synthetic triazole derivative structurally related to fluconazole, antifungal Terconazole seems to disrupt cell wall synthesis by inhibiting biosynthesis of ergosterol or other sterols, damaging the fungal cell membrane, altering its permeability, and promoting loss of essential intracellular elements. Terconazole is active against Candida sp.

2,6-Dichlorodiphenylamine, an analogue of Diclofenac Sodium, exhibits anti-Candida albicans activity. Diclofenac Sodium, a potent and nonselective COX inhibitor, has IC50 values of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells. [1]. Makoto Urai, et al. Potent Drugs That Attenuate anti-Candida albicans Activity of Fluconazole and Their Possible Mechanisms of Action. J Infect Chemother. 2014 Oct;20(10):612-5.

3-AMINO-1,2,4-TRIAZINE is an aromatic bioactive compound. It has been used to synthesize a variety of drugs, including the antifungal drug fluconazole, the anti-inflammatory drug ibuprofen and the anticancer drug paclitaxel. It has also been used in the design of new drugs, such as the anti-AIDS drug zidovudine and the anti-malarial drug artemisinin.

CYP51-IN-9 (compound 1i) is an analog of Fluconazole and serves as an effective antifungal agent. It exhibits a MIC80 of 62.5 ng mL against Microsporum gypseum and Candida albicans, indicating potent inhibitory activity.

CYP51-IN-12 (compound 1l), an analog of Fluconazole, serves as an effective antifungal agent. It inhibits Microsporum gypseum and Candida albicans with a MIC80 of 15.6 ng mL.

CYP51-IN-7 (compound 1g) is an analogue of Fluconazole and serves as an effective antifungal agent. It exhibits inhibitory activity against Microsporum gypseum and Candida albicans, with MIC80 values of 62.5 ng mL and 250 ng mL, respectively.

CYP51-IN-14 (compound 1n), a derivative of Fluconazole, functions as an effective antifungal agent. This compound inhibits Microsporum gypseum and Candida albicans with a minimum inhibitory concentration (MIC80) of 1 μg mL.

CYP51-IN-13 (compound 1m), a fluconazole analog, serves as an effective antifungal agent. It inhibits Microsporum gypseum and Candida albicans with MIC80 values of 62.5 ng mL and 250 ng mL, respectively.

CYP51-IN-4 (compound 1d), an analog of Fluconazole, serves as an effective antifungal agent. It inhibits Microsporum gypseum and Candida albicans with an MIC80 of 15.6 ng mL.

CYP51-IN-8 (compound 1h), an analog of Fluconazole, serves as an effective antifungal agent. It inhibits Microsporum gypseum and Candida albicans with MIC80 values of 15.6 and 62.5 ng mL, respectively.

CYP51-IN-6 (compound 1f) is an analog of Fluconazole and serves as an effective antifungal agent. It inhibits Microsporum gypseum and Candida albicans with MIC80 values of 62.5 and 15.6 ng mL, respectively.

CYP51-IN-2 (compound 1b), a Fluconazole analog, serves as a potent antifungal agent. It exhibits activity against Gypseum and Candida Albicans that is 64 and 128 times higher, respectively, compared to Fluconazole.

ZD 0870, used to treat infections caused by fluconazole-resistant candida albicans.

Milbemycin A4 oxime, a derivative of milbemycin A4 and a component of milbemycin oxime, exhibits insecticidal and nematocidal activity. At 0.05 mg kg, it reduces microfilariae of the heartworm D. immitis in naturally infested dogs and inhibits the growth of C. glabrata clinical isolates with MIC80 values of 16 to >32 μg ml. At 2.5 μg ml, it blocks fluconazole efflux from C. glabrata clinical isolates (but not from strains lacking CgCDR1 and PDH1 efflux pumps) and reduces MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. Furthermore, it enhances adriamycin-induced inhibition of cell growth, increases intracellular accumulation of adriamycin and the P-glycoprotein substrate rhodamine 123 in adriamycin-resistant, but not adriamycin-sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.

Chitin synthase inhibitor 2 (compound 2b) is a highly potent inhibitor of chitin synthase, with an IC50 of 0.09 mM and a K i of 0.12 mM. This compound exhibits antimicrobial activity in vitro and demonstrates synergistic or additive effects when combined with fluconazole or polyoxin B [1].

Antifungal agent 28 (compound 18) is a selective and potent antifungal agent that disrupts mature Candida biofilms and inhibits pathogenic strains of Candida albicans and non-Candida albicans, including fluconazole-resistant strains.

BI-10 is an antifungal compound that, in combination with fluconazole, inhibits mycelial growth, accumulates ROS, reduces mitochondrial membrane potential (MMP) and alters membrane permeability.