Significant improvement of antifungal activity of polyene macrolides by bisalkylation of the mycosamine

被引：59
作者：
Paquet, V [1 ]
Carreira, EM [1 ]
机构：
[1] ETH Honggerberg, Organ Chem Lab, CH-8093 Zurich, Switzerland
来源：
ORGANIC LETTERS | 2006年 / 8卷 / 09期
关键词：
D O I：
10.1021/ol060353o
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
New derivatives of Amphotericin 8 (AmB) were synthesized through a double reductive alkylation of the mycosamine. These derivatives of AmB displayed superior antifungal activity against Saccharomyces cerevisiae wild-type strain and especially in the case of an AmB-resistant Candida albicans strain. Moreover, these compounds are potential drug candidates because of significantly reduced hemotoxicity compared to AmB. Furthermore, the same mycosamine modification can be applied to other polyene macrolides such as Nystatin and Pimaricin to improve their antifungal activity.
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页码：1807 / 1809
页数：3
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