ketoconazole

Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

(-)-Ketoconazole is one of the enantiomer of Ketoconazole. Ketoconazole is a racemic mixture of two enantiomers.

(+)-Ketoconazole ((+)-R 41400) is a broad-spectrum oral antifungal compound, a CYP3A4 inhibitor, used for the study of fungal infections and seborrheic dermatitis.

Ketoconazole Intermediate 1e ((cis-2-((1H-Imidazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methyl 4- methylbenzenesulfonate) is a ketoconazole intermediate.

Deacylketoconazole (Deacyl ketoconazole) is a Ketoconazole derivative and is also an antifungal agent. Deacylketoconazole was 15- to 50-fold more active against Plasmodium falciparum than was ketoconazole.

TG-100435 is a novel multi-target oral protein tyrosine kinase inhibitor. The metabolic flux of TG100435 is entirely inhibited by methimazole and ketoconazole. In human liver microsomes or recombinant P450, the formation of TG100435 increases with the activity of cytochrome P450 reductase, suggesting that cytochrome P450 reductase may be involved.

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.

(±)17(18)-EpETE-Ethanolamide, an ω-3 endocannabinoid epoxide, originates from eicosapentaenoic ethanolamide (EPEA) through cytochrome P450 (CYP) epoxygenases action and is decomposed by soluble epoxide hydrolase (sEH) and fatty acid amide hydrolase (FA, AH). Its endogenous synthesis occurs in LPS-stimulated and EPEA-supplemented BV-2 microglia cells, a process inhibited by the CYP inhibitor ketoconazole. This compound mitigates IL-6 and nitrite levels while enhancing IL-10 production following LPS exposure in BV-2 microglia. At a dose of 50 µM, it prevents platelet aggregation caused by arachidonic acid but not that triggered by ADP, collagen, or ristocetin. Additionally, it facilitates the dilation of constricted bovine coronary arteries (ED50= 1.1 µM) and blocks VEGF-driven tubulogenesis in human microvascular endothelial cells (HMVECs).

Eberconazole, a dichlorinated imidazole derivative, exhibits antifungal activity and outperforms Clotrimazole, Ketoconazole, and Miconazole in efficacy. It holds promise for dermatophytoses research through topical administration.

Eberconazole Nitrate (Ebernet) is an azole antifungal agent and broad-spectrum imidazole derivative.