Authors: Thevissen, Karin; Marchand, Arnaud; Chaltin, Patrick; Meert, Els M.K.; Cammue, Bruno P.A.

Source: Current Medicinal Chemistry, Volume 16, Number 17, June 2009 , pp. 2205-2211(7)

Publisher: Bentham Science Publishers

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 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

Document Type: Research article

DOI: http://dx.doi.org/10.2174/092986709788612701

Affiliations: 1: CMPG, K.U. Leuven, Kasteelpark Arenberg 20, 3001 Heverlee, Belgium.

Publication date: 2009-06-01

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• Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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