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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Bibliographic Details
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
Subjects:	Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Aspergillus niger Biological and medical sciences Candida albicans Cryptococcus albidus Medical sciences Pharmacology. Drug treatments Fungi Candida albicans Antifungal agent Sensitivity resistance Enzyme Enzyme inhibitor Fungi Imperfecti In vitro Clinical isolate Thallophyta
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Summary:	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.
Bibliography:	ObjectType-Article-2 SourceType-Scholarly Journals-1 ObjectType-Feature-1 content type line 23
ISSN:	0305-7453 1460-2091
DOI:	10.1093/jac/39.2.261