Synthesis and in vitro evaluation of novel highly potent coumarin inhibitors of gyrase B

Authors
Laurin, P Ferroud, D Klich, M Dupuis-Hamelin, C Mauvais, P Lassaigne, P Bonnefoy, A Musicki, B
Citation
P. Laurin et al., Synthesis and in vitro evaluation of novel highly potent coumarin inhibitors of gyrase B, BIOORG MED, 9(14), 1999, pp. 2079-2084
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
14
Year of publication
1999
Pages
2079 - 2084
Database
ISI
SICI code
0960-894X(19990719)9:14<2079:SAIVEO>2.0.ZU;2-1
Abstract
The design, synthesis, and in vitro biological activity of a series of nove l coumarin inhibitors of gyrase B is presented. Replacement of the 3-acylam ino residue (3-NHCOR) of coumarin drugs with reversed isosteres C(=O)R, C(= N-OR)R', COOR, CONHR and CONHOR leads to highly potent analogues which disp layed excellent inhibition of the negative supercoiling of the relaxed DNA and antibacterial activity. (C) 1999 Elsevier Science Ltd. All rights reser ved.