title: Novel antifungal agents which inhibit lanosterol 14alpha-demethylase in Candida albicans CCH442.
abstract: We have identified four non-azole inhibitors of lanosterol 14a-demethylase in Candida albicans CCH442. The most potent compound, A-39806, had IC50 values for ergosterol inhibition of 0.9 microM (0.3 mg/L) and 1.9 microM (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.
authors.affiliation: Anti-infective Research Division, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
authors.forename: D
authors.initials: D
authors.lastname: Zakula
authors.forename: J O
authors.initials: JO
authors.lastname: Capobianco
authors.forename: R C
authors.initials: RC
authors.lastname: Goldman
mesh_terms: D000935:Antifungal Agents / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects* / Q000201:enzymology; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D010088:Oxidoreductases / Q000037:antagonists & inhibitors*; D058886:Sterol 14-Demethylase
chemical_list: D000935:Antifungal Agents; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D010088:Oxidoreductases; D058886:Sterol 14-Demethylase