title: Antifungal carbazoles.
abstract: Carbazole derivatives are well known for their various pharmacological activities, including anti-HIV, anticancer, antibacterial and antifungal activities. This review will focus on carbazoles that possess antifungal activity against Candida albicans, the major human fungal pathogen. In our search for new fungicidal compounds, we identified a series of substituted carbazoles, termed N-alkylated 3,6-dihalogenocarbazoles, that exhibit fungicidal activity against C. albicans and the emerging pathogen Candida glabrata. The most potent fungicidal compounds of this series were characterized by minimal fungicidal concentration (MFC) between 8.5 and 25 microM. To analyse the structural determinants for fungicidal activity of these carbazole derivatives, we selected 10 such derivatives and performed further analyses. Interestingly, some of these N-alkaylated 3,6-dihalogenocarbazoles were active against Candida biofilms grown in microtiterplates. In this review, we will further discuss the putative therapeutic potential of the antifungal carbazole compounds as antimycotics.
authors.affiliation: CMPG, K.U. Leuven, Kasteelpark Arenberg 20, 3001 Heverlee, Belgium. karin.thevissen@biw.kuleuven.be
authors.forename: Karin
authors.initials: K
authors.lastname: Thevissen
authors.forename: Arnaud
authors.initials: A
authors.lastname: Marchand
authors.forename: Patrick
authors.initials: P
authors.lastname: Chaltin
authors.forename: Els M K
authors.initials: EM
authors.lastname: Meert
authors.forename: Bruno P A
authors.initials: BP
authors.lastname: Cammue
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D018441:Biofilms / Q000187:drug effects / Q000254:growth & development; D002227:Carbazoles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D015195:Drug Design; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009181:Mycoses / Q000188:drug therapy*; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D002227:Carbazoles