Novel antifungal agents which inhibit lanosterol 14α-demethylase in Candida albicans CCH442

We have identified four non-azole inhibitors of lanosterol 14 alpha -demethylase in Candida albicans CCH442. The most potent compound, A-39806, had IC sub(50) values for ergosterol inhibition of 0.9 mu M (0.3 mg/L) and 1.9 mu M (0.6 mg/L) in whole cell and cell-free extract assays, respectively. A-3...

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Published in:Journal of antimicrobial chemotherapy Vol. 39; no. 2; pp. 261 - 264
Main Authors: ZAKULA, D, CAPOBIANCO, J. O, GOLDMAN, R. C
Format: Journal Article
Language:English
Published: Oxford Oxford University Press 01-02-1997
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Abstract We have identified four non-azole inhibitors of lanosterol 14 alpha -demethylase in Candida albicans CCH442. The most potent compound, A-39806, had IC sub(50) values for ergosterol inhibition of 0.9 mu M (0.3 mg/L) and 1.9 mu M (0.6 mg/L) in whole cell and cell-free extract assays, respectively. A-39806 demonstrated broad in-vitro antifungal activity against several Candida species as well as against Cryptococcus albidus and Aspergillus niger. In-vitro antifungal activity was also demonstrated against a fluconazole-resistant clinical isolate of C. albicans.
AbstractList We have identified four non-azole inhibitors of lanosterol 14 alpha -demethylase in Candida albicans CCH442. The most potent compound, A-39806, had IC sub(50) values for ergosterol inhibition of 0.9 mu M (0.3 mg/L) and 1.9 mu M (0.6 mg/L) in whole cell and cell-free extract assays, respectively. A-39806 demonstrated broad in-vitro antifungal activity against several Candida species as well as against Cryptococcus albidus and Aspergillus niger. In-vitro antifungal activity was also demonstrated against a fluconazole-resistant clinical isolate of C. albicans.
Author GOLDMAN, R. C
ZAKULA, D
CAPOBIANCO, J. O
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  organization: Anti-infective Research Division, Abbott Laboratories, One Abbott Park Road, Abbott Park, IL 60064-3500, United States
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Keywords Fungi
Candida albicans
Antifungal agent
Sensitivity resistance
Enzyme
Enzyme inhibitor
Fungi Imperfecti
In vitro
Clinical isolate
Thallophyta
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Snippet We have identified four non-azole inhibitors of lanosterol 14 alpha -demethylase in Candida albicans CCH442. The most potent compound, A-39806, had IC sub(50)...
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SubjectTerms Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal agents
Aspergillus niger
Biological and medical sciences
Candida albicans
Cryptococcus albidus
Medical sciences
Pharmacology. Drug treatments
Title Novel antifungal agents which inhibit lanosterol 14α-demethylase in Candida albicans CCH442
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