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Literature DB >> 490531

Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent.

J Heeres, L J Backx, J H Mostmans, J Van Cutsem.

Abstract

The preparation and antifungal properties of cis-1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-yl-methyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazine (I) are described. Ketoconazole has, at low oral doses, a high in vivi activity against vaginal candidosis in rats and against cutaneous candidosis in guinea pigs.

Entities: Chemical Disease Gene Species

Mesh：

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Year: 1979 PMID： 490531 DOI： 10.1021/jm00194a023

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

31 in total

1. Antiproliferative effects and mechanism of action of ICI 195,739, a novel bis-triazole derivative, on epimastigotes and amastigotes of Trypanosoma (Schizotrypanum) cruzi.

Authors: J A Urbina; K Lazardi; T Aguirre; M M Piras; R Piras
Journal: Antimicrob Agents Chemother Date: 1991-04 Impact factor: 5.191

Review 2. Drug repurposing for the treatment of COVID-19: Pharmacological aspects and synthetic approaches.

Authors: Pedro N Batalha; Luana S M Forezi; Carolina G S Lima; Fernanda P Pauli; Fernanda C S Boechat; Maria Cecília B V de Souza; Anna C Cunha; Vitor F Ferreira; Fernando de C da Silva
Journal: Bioorg Chem Date: 2020-11-19 Impact factor: 5.275

3. Ultrastructural alterations induced by two ergosterol biosynthesis inhibitors, ketoconazole and terbinafine, on epimastigotes and amastigotes of Trypanosoma (Schizotrypanum) cruzi.

Authors: K Lazardi; J A Urbina; W de Souza
Journal: Antimicrob Agents Chemother Date: 1990-11 Impact factor: 5.191

4. Inhibition of CYP3A4 and CYP3A5 catalyzed metabolism of alprazolam and quinine by ketoconazole as racemate and four different enantiomers.

Authors: Annika Allqvist; Jun Miura; Leif Bertilsson; Rajaa A Mirghani
Journal: Eur J Clin Pharmacol Date: 2007-01-03 Impact factor: 2.953

10. Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.

Authors: J E Parker; M Merkamm; N J Manning; D Pompon; S L Kelly; D E Kelly
Journal: Antimicrob Agents Chemother Date: 2008-08-11 Impact factor: 5.191

Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent.

1. Antiproliferative effects and mechanism of action of ICI 195,739, a novel bis-triazole derivative, on epimastigotes and amastigotes of Trypanosoma (Schizotrypanum) cruzi.

Review 2. Drug repurposing for the treatment of COVID-19: Pharmacological aspects and synthetic approaches.

3. Ultrastructural alterations induced by two ergosterol biosynthesis inhibitors, ketoconazole and terbinafine, on epimastigotes and amastigotes of Trypanosoma (Schizotrypanum) cruzi.

4. Inhibition of CYP3A4 and CYP3A5 catalyzed metabolism of alprazolam and quinine by ketoconazole as racemate and four different enantiomers.

Review 5. An overview of topical antifungal therapy in dermatomycoses. A North American perspective.

6. Organism-dependent fungicidal activities of azoles.

7. Hematogenous Candida vertebral osteomyelitis treated with ketoconazole.

8. Distribution of oral ketoconazole to vaginal tissue.

9. In vitro and in vivo effects of the antimycotic drug ketoconazole on sterol synthesis.

10. Differential azole antifungal efficacies contrasted using a Saccharomyces cerevisiae strain humanized for sterol 14 alpha-demethylase at the homologous locus.