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

Authors
Masubuchi, M Kawasaki, K Ebiike, H Ikeda, Y Tsujii, S Sogabe, S Fujii, T Sakata, K Shiratori, Y Aoki, Y Ohtsuka, T Shimma, N
Citation
M. Masubuchi et al., Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1, BIOORG MED, 11(14), 2001, pp. 1833-1837
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
14
Year of publication
2001
Pages
1833 - 1837
Database
ISI
SICI code
0960-894X(20010723)11:14<1833:DASONB>2.0.ZU;2-9
Abstract
Potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibi tors have been identified through optimization of a lead compound 1 discove red by random screening. The inhibitor design is based on the crystal struc ture of the CaNmt complex with compound (S)-3 and structure-activity relati onships (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.