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Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lebouvier N,Pagniez F,Duflos M,Le Pape P,Na YM,Le Baut G,Le Borgne M

doi

10.1016/j.bmcl.2007.04.038

subject

Has Abstract

pub_date

2007-07-01 00:00:00

pages

3686-9

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00458-1

journal_volume

17

pub_type

杂志文章

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