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

被引：80

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.

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页码：607 / 610

页数：4

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