Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase.: Part 2

被引：79
|
作者：
Ebiike, H
Masubuchi, M
Liu, PL
Kawasaki, K
Morikami, K
Sogabe, 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, Kanagawa 2478530, Japan
[2] Nippon Roche Res Ctr, Dept Mycol, Kanagawa 2478530, Japan
[3] Nippon Roche Res Ctr, Dept Preclin Sci, Kamakura, Kanagawa 2478530, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 04期
关键词：
D O I：
10.1016/S0960-894X(01)00808-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Modification of the C-2 position of a benzofuran derivative 6 (RO-09-4609), an N-myristoyltransferase (Nmt) inhibitor, has led us to discover antifungal agents that are active in a murine systemic candidiasis model. The drug design is based on the analysis of a crystal structure of a Candida Nmt complex with 2. The optimization has been guided by various biological evaluations including a quasi in vivo assay and pharmacokinetic analysis. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：607 / 610
页数：4
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