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. 2007 Jul 1;17(13):3686-9.
doi: 10.1016/j.bmcl.2007.04.038. Epub 2007 Apr 19.

Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety

Nicolas Lebouvier  1 , Fabrice Pagniez, Muriel Duflos, Patrice Le Pape, Young Min Na, Guillaume Le Baut, Marc Le Borgne
Affiliations

Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety

Nicolas Lebouvier et al. Bioorg Med Chem Lett. .

Abstract

A series of fluconazole analogues 5-20 incorporating azaindole and indole moieties were prepared using oxirane intermediates synthesized under microwave irradiation. All of the compounds were evaluated in vitro against two clinically important fungi, Candida albicans and Aspergillus fumigatus. Four derivatives 6, 13, 14 and 18 exerted high antifungal activity against C. albicans with MIC(80) values 3- to 28-fold lower than that of fluconazole.

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