Antifungal Ketoconazole Raw Materials powder

CAS:65277-42-1

MF:C26H28Cl2N4O4

MW:531.43

EINECS:265-667-4

Specification: 99% min Ketoconazole powder

Sample:Ketoconazole powder

Packaging:1kg/bag, 25kg/drum

From:Henrikang

Appearance:white

Shelf Life: 2 Years

Test Method: HPLC

Ketoconazole powder Usage and Synthesis.

Ketoconazole is indicated for the treatment of the following systemic fungal infections:

1. Candidiasis, chronic cutaneous mucosal candidiasis, oral candidiasis, urinary tract candidiasis, chronic, recurrent vaginal candidiasis that does not respond to local treatment. 2. Dermatitis blastomycosis. 3. Coccidioidomycosis.

4. Histoplasmosis.

5. Pigmented mycosis.

6. Paraccidioidomycosis. Dermatomycosis, tinea versicolor and tinea tinea caused by skin fungi and yeast can be treated with this product when local treatment or oral griseofulvin does not work, or when severe intractable skin fungal infections are difficult to receive griseofulvin treatment.

Uses of Ketoconazole powder.

Ketoconazole is used in the treatment of candidiasis, chronic mucocutaneous candidiasis, thrush, candidiasis, blastomycosis, coccidioidomycosis, histoplasmosis, chromosomal mycosis and paracoccidioidomycosis. Itis is used to identify p-glycoprotein/CYP3A-restricted bioavailability in their key models to study interleukin-1-mediated antitumor effects, and drug-drug interactions in vivo.

Pharmacological action of Ketoconazole.

1. Pharmacology Ketoconazole is a pyrrole antifungal drug, which has antibacterial effect on deep infection fungi such as Candida, pigmentomyces, coccidioides, histoplasmosis, Sporotrichophyton, etc. It also has antibacterial activity against trichophyton trichophyton. It has weak effect on Aspergillus, Sporotrichothrix Schenckii, some melanosporaceae and Mucor. By interfering with the activity of cytochrome P-450, this product inhibits the biosynthesis of ergosterol, the main sterol in fungal cell membranes, damages fungal cell membranes and changes their permeability, resulting in the leakage of important intracellular substances. Ketoconazole can inhibit the biosynthesis of triacylglycerol and phospholipids of fungi, inhibit the activity of oxidase and peroxidase, and cause intracellular hydrogen peroxide accumulation leading to cell submicrostructure degeneration and cell necrosis. Candida albicans can inhibit the process of its transformation from spore to aggressive mycelium.

2. Toxicology animal long-term toxicity experiments show that ketoconazole can significantly increase alkaline phosphatase and denature liver cells.

Product method of Bulk Ketoconazole powder.

The mixture of 2.4 parts 1-acetyl -4- (4-hydroxybenzene) piperazine, 0.4 parts 78% sodium hydride, 75 parts dimethyl sulfate and 22.5 parts benzene was stirred at 40℃ for 1h, and then 4.2 parts 2- (2, 4-dichlorobenzene -2- (1h-imidazole-1-methyl) -1, 3-dioxopentyl environmental protection -4-methyl mesylate was added. Stir at 100 ° C overnight. The reaction product was post-treated to obtain 3.2 parts ketoconazole.