Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase.: Part 1

被引：101

作者：

Masubuchi, M ^{[1
]}

Kawasaki, K ^{[1
]}

Ebiike, H ^{[1
]}

Ikeda, Y ^{[1
]}

Tsujii, S ^{[1
]}

Sogabe, S ^{[1
]}

Fujii, T ^{[1
]}

Sakata, K ^{[1
]}

Shiratori, Y ^{[1
]}

Aoki, Y ^{[1
]}

Ohtsuka, T ^{[1
]}

Shimma, N ^{[1
]}

机构：

[1] Nippon Roche Res Ctr, Kamakura, Kanagawa 2478530, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(01)00319-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitors have been identified through optimization of a lead compound 1 discovered by random screening. The inhibitor design is based on the crystal structure of the CaNmt complex with compound (S)-3 and structure-activity relationships (SARs) have been clarified. Modification of the C-4 side chain of 1 has led to thr discovery of a potent and selective CaNmt inhibitor 11 (RO-09-4609), which exhibits antifungal activity against C. albicans in vitro, (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1833 / 1837

页数：5

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