二芳基脒衍生物的抗真菌和抗菌活性。
Antifungal and antibacterial activities of diarylamidine derivatives.
作者信息
Anné J, De Clercq E, Eyssen H, Dann O
出版信息
Antimicrob Agents Chemother. 1980 Aug;18(2):231-9. doi: 10.1128/AAC.18.2.231.
Abstract
The antifungal and antibacterial properties of a series of 70 diarylamidine derivatives were evaluated. Several of these compounds exhibited considerable antimicrobial potency. A survey of the structure-activity relationship demonstrated that minor structural variations resulted in significant changes of antimicrobial activity. In general, the structural features required for antifungal activity coincided with those required for antibacterial activity. Both the antifungal and the antibacterial properties of the diarylamidines depended on the presence and the positions, of both amidino groups, on the nature of the central bridge connecting the two aryl moieties, and on the nature of these aryl residues (preferably indole). The most active compound was evaluated for its activity against Candida albicans infection in mice.
摘要
对一系列70种二芳基脒衍生物的抗真菌和抗菌特性进行了评估。其中几种化合物表现出相当强的抗菌效力。对构效关系的研究表明，微小的结构变化会导致抗菌活性的显著改变。一般来说，抗真菌活性所需的结构特征与抗菌活性所需的特征一致。二芳基脒的抗真菌和抗菌特性均取决于脒基的存在和位置、连接两个芳基部分的中心桥的性质以及这些芳基残基（最好是吲哚）的性质。对活性最强的化合物进行了针对小鼠白色念珠菌感染的活性评估。
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