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.

引用

页码：87 / 91

页数：5

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