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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Antifungal Carbazoles

Author(s): Karin Thevissen, Arnaud Marchand, Patrick Chaltin, Els M.K. Meert and Bruno P.A. Cammue

Volume 16, Issue 17, 2009

Page: [2205 - 2211] Pages: 7

DOI: 10.2174/092986709788612701

Price: $65


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 μM. 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.

Keywords: Carbazoles, Candida sp., fungicidal, structure activity relationship, fungal biofilm

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