(2-arylhydrazonomethyl)-substituted xanthones as antimycotics:: synthesis and fungistatic activity against Candida species

被引：22

作者：

Moreau, S ^{[1
]}

Verache-Lembège, M ^{[1
]}

Larrouture, S ^{[1
]}

Fall, D ^{[1
]}

Neveu, A ^{[1
]}

Deffieux, G ^{[1
]}

Vercauteren, J ^{[1
]}

Nuhrich, A ^{[1
]}

机构：

[1] Univ Victor Segalen Bordeaux 2, Grp Etud Subst Nat Interet Therapeut GESNIT, EA 491, F-33076 Bordeaux, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 37卷 / 03期

关键词：

arylhydrazono-xanthones; synthesis; structural study; in vitro anticandida activity;

D O I：

10.1016/S0223-5234(01)01332-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of arylhydrazones derived from various 6,8-diacetoxy- or 6,8-dihydroxy-9-oxo-9H-xanthene carboxaldehydes were synthesized and evaluated for their in vitro antifungal properties against two human pathogenic yeasts (Candida albicans and C. krusei) according to a diffusion method. The activity was strongly dependent from the position of the (1-arylhydrazinyl-2-ylidene)methyl chain in the xanthone molecular skeleton. Compounds having the nitrogen side chain in the 4-position, with a further halogen substitution on the terminal phenyl ring showed fungistatic effects. Within this series, the 4-fluorophenylhydrazinyl derivative 13g exhibited the highest activity, particularly against C. krusei, with a greater efficacy than that of econazole, used as reference. (C) 2002 Published by Editions scientifiques et medicales Elsevier SAS.

引用

页码：237 / 253

页数：17

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