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(+)-Ketoconazole

CAS No. : 142128-59-4

Biological Activity：(+)-Ketoconazole ((+)-R 41400) is an imidazole anti-fungal agent, a CYP3A4 inhibitor.
Target: CYP3A4
(+)-Ketoconazole, an imidazole anti-fungal agent, has often produced features of androgen deficiency including decreased libido, gynecomastia, impotence, oligospermia, and decreased testosterone levels, in men being treated for chronic mycotic infections [1]. (+)-Ketoconazole also is a cytochrome P450 inhibitor [2].
(+)-Ketoconazole (KTZ), on the antischistosomal potential of these quinolines against Schistosoma mansoni infection by evaluating parasitological, histopathological, and biochemical parameters. Mice were classified into 7 groups: uninfected untreated (I), infected untreated (II), infected treated orally with PZQ (1,000 mg/kg) (III), QN (400 mg/kg) (IV), KTZ (10 mg/kg)+QN as group IV (V), HF (400 mg/kg) (VI), and KTZ (as group V)+HF (as group VI) (VII). KTZ plus QN or HF produced more inhibition (P<0.05) in hepatic CYP450 (85.7% and 83.8%) and CYT b5 (75.5% and 73.5%) activities, respectively, than in groups treated with QN or HF alone. This was accompanied with more reduction in female (89.0% and 79.3%), total worms (81.4% and 70.3%), and eggs burden (hepatic; 83.8%, 66.0% and intestinal; 68%, 64.5%), respectively, and encountering the granulomatous reaction to parasite eggs trapped in the liver [3]. Clinical indications: Candida infection; Dermatophytosis; Folliculitis FDA Approved Date: Toxicity: teratogenesis; liver injuries; adrenal gland problems

Research Area：Infection

Targets：Fungal|Cytochrome P450

Related Screening Libraries:Drug Repurposing Compound Library Plus;FDA-Approved Drug Library Plus;FDA-Approved Drug Library Mini;Bioactive Compound Library Plus;Anti-Infection Compound Library;Metabolism/Protease Compound Library;FDA-Approved Drug Library;Anti-Aging Compound Library;Drug Repurposing Compound Library;Antioxidant Compound Library;Oxygen Sensing Compound Library;Antifungal Compound Library;Orally Active Compound Library;FDA Approved & Pharmacopeial Drug Library;

Related Small Molecules:Antifungal agent 20;SR9186;AMG-208;Debneyol;Haloprogin;Staurosporine;Ciclopirox-d11;Ciclopirox olamine;Clotrimazole-d5;(R)-Camptothecin-d5;Ticlatone;Aminothiazole;Magnesium silicate;CYP1B1-IN-1;CYP2C9/CYP2C19-IN-1;α-Terpinene;Hydroxyphenyllactic acid;Iprobenfos;Hypericin;Chlorphenesin;Moniliformin sodium salt;HLF1-11;β-Amyrin acetate;Bifonazole

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