Synthesis and anfifungal activities of new fluconazole analogues with azaheterocycle moiety

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 MIC80 values 3- to 28-fold lower than that of fluconazole. (c) 2007 Elsevier Ltd. All rights reserved.