Synthesis and antibacterial properties of beta-diketone acrylate bioisosteres of pseudomonic acid A

Authors
Bennett, I Broom, NJP Cassels, R Elder, JS Masson, ND O'Hanlon, PJ
Citation
I. Bennett et al., Synthesis and antibacterial properties of beta-diketone acrylate bioisosteres of pseudomonic acid A, BIOORG MED, 9(13), 1999, pp. 1847-1852
Citations number
7
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
13
Year of publication
1999
Pages
1847 - 1852
Database
ISI
SICI code
0960-894X(19990705)9:13<1847:SAAPOB>2.0.ZU;2-Z
Abstract
A series of beta-diketone acrylate bioisosteres 4 of pseudomonic acid A 1 h ave been synthesized and evaluated for their ability to inhibit bacterial i soleucyl-tRNA synthetase and act as antibacterial agents. A number of analo gues have excellent antibacterial activity. Selected examples were shown to afford good blood levels and to be effective in a murine infection model. (C) 1999 Elsevier Science Ltd. All rights reserved.