Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase.: Part 3

被引：99
|
作者：
Kawasaki, K
Masubuchi, M
Morikami, K
Sogabe, S
Aoyama, T
Ebiike, H
Niizuma, S
Hayase, M
Fujii, T
Sakata, K
Shindoh, H
Shiratori, Y
Aoki, Y
Ohtsuka, T
Shimma, N
机构：
[1] Nippon Roche Res Ctr, Dept Chem, Kamakura, Kanagawa 2478530, Japan
[2] Nippon Roche Res Ctr, Dept Mycol, Kamakura, Kanagawa 2478530, Japan
[3] Nippon Roche Res Ctr, Dept Preclin Sci, Kamakura, Kanagawa 2478530, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 01期
关键词：
D O I：
10.1016/S0960-894X(02)00844-2
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new series of acid-stable antifungal agents having strong inhibitory activity against Candida albicans N-myristoyl-transferase (CaNmt) has been developed starting from acid-unstable benzofuranylmethyl aryl ether 2. The inhibitor design is based on X-ray crystallographic analysis of a CaNmt complex with aryl ether 3. Among the new inhibitors, pyridine derivative 8b and benzimidazole derivative 8k showed clear antifungal activity in a murine systemic candidiasis model. (C) 2002 Elsevier Science Ltd. All rights reserved.
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收藏
页码：87 / 91
页数：5
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