Analogues of SB-203207 as inhibitors of tRNA synthetases

Authors
Banwell, MG Crasto, CF Easton, CJ Forrest, AK Karoli, T March, DR Mensah, L Nairn, MR O'Hanlon, PJ Oldham, MD Yue, WM
Citation
Mg. Banwell et al., Analogues of SB-203207 as inhibitors of tRNA synthetases, BIOORG MED, 10(20), 2000, pp. 2263-2266
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
20
Year of publication
2000
Pages
2263 - 2266
Database
ISI
SICI code
0960-894X(20001016)10:20<2263:AOSAIO>2.0.ZU;2-#
Abstract
SB-203207 and 10 analogues have been prepared, by elaboration of altemicidi n, and evaluated as inhibitors of isoleucyl, leucyl and valyl tRNA syntheta ses (IRS, LRS, and VRS, respectively). Substituting the isoleucine residue of SB-203207 with leucine and valine increased the potency of inhibition of LRS and VRS, respectively. The leucine derivative showed low level antibac terial activity, while several of the compounds inhibited IRS from Staphylo coccus aureus WCUH29 more strongly than rat liver IRS. (C) 2000 Elsevier Sc ience Ltd. All rights reserved.