Synthesis and HIV-1 integrase inhibitory activities of catechol and bis-catechol derivatives

Authors
Dupont, R Jeanson, L Mouscadet, JF Cotelle, P
Citation
R. Dupont et al., Synthesis and HIV-1 integrase inhibitory activities of catechol and bis-catechol derivatives, BIOORG MED, 11(24), 2001, pp. 3175-3178
Citations number
25
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
24
Year of publication
2001
Pages
3175 - 3178
Database
ISI
SICI code
0960-894X(200112)11:24<3175:SAHIIA>2.0.ZU;2-5
Abstract
Fourteen catechol and bis-catechol derivatives have been synthesised and te sted for their HIV-1 inhibitory activities. The six more active molecules h ave been tested for their antiviral activity and cytotoxicity. We have foun d that bis-catechols 1 and 2 are the most active HIV-1 integrase inhibitor whereas the best antiviral compound is 4. (C) 2001 Elsevier Science Ltd. Al l rights reserved.