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源自2-(2,4-二氯苯基)-1,3-二氧戊环的新型聚唑衍生物。抗真菌活性。构效关系。

New polyazole derivatives from 2-(2,4-dichlorophenyl)-1,3-dioxolane. Antifungal activity. Structure-activity relationships.

作者信息

Delcourt A, Mathieu G, Baji H, Kimny T, Flammang M, Compagnon P L

机构信息

Laboratoire de Botanique et de Cryptogamie, Faculté de Pharmacie, Dijon, France.

出版信息

Mycopathologia. 1997;137(1):27-32. doi: 10.1023/a:1006837606890.

Abstract

Six new polyazole derivatives from 2-(2,4-dichlorophenyl)-1,3-dioxolane were studied for their antifungal activity against pathogenic fungi for humans and animals. The antimycotic effect was largely restricted to the filamentous fungi with Aspergillus fumigatus and Scedosporium apiospermum being remarkably susceptible. Three compounds were as effective as the two references, ketoconazole and oxiconazole. The structure-activity relationships revealed than an 'oxime group' combined with four chlorine atoms increased the antifungal properties of the chemical series.

摘要

对六种源自2-(2,4-二氯苯基)-1,3-二氧戊环的新型聚唑衍生物进行了研究,考察它们对人类和动物致病真菌的抗真菌活性。抗真菌作用主要局限于丝状真菌,烟曲霉和尖端赛多孢菌对其尤为敏感。三种化合物的效果与酮康唑和奥昔康唑这两种对照药相当。构效关系表明,一个“肟基”与四个氯原子相结合可增强该化学系列的抗真菌性能。

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