Synthesis of sordaricin analogues as potent antifungal agents against Candida albicans

被引：14
作者：
Kaneko, S
Uchida, T
Shibuya, S
Honda, T
Kawamoto, I
Harasaki, T
Fukuoka, T
Konosu, T
机构：
[1] Sankyo Co Ltd, Med Chem Res Labs, Shinagawa Ku, Tokyo 1408710, Japan
[2] Sankyo Co Ltd, Biol Res Labs, Shinagawa Ku, Tokyo 1408710, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 05期
关键词：
D O I：
10.1016/S0960-894X(02)00020-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Sordaricin derivatives possessing a cyclohexane ring appendage attached via an ether. thioether. amine, oxime. ester or amide linkage were synthesized and their antifungal activity was evaluated in vitro. Compounds containing a thioether bond or an oxime bond as a linkage exhibited potent MICs (less than or equal to0.125 mug/mL) against four Candida albicans strains including azole-low-susceptible strains. They were also active (MIC less than or equal to0.125 mug/mL) against Candida glabrata. Their in vivo efficacy was confirmed in a murine intravenous infection model with Candida albicans. (C) 2002 Elsevier Science Ltd. All rights reserved.
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收藏
页码：803 / 806
页数：4
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