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

R Dupont; L Jeanson; J F Mouscadet; P Cotelle

doi:10.1016/s0960-894x(01)00658-8

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

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3175-8. doi: 10.1016/s0960-894x(01)00658-8.

Authors

R Dupont¹, L Jeanson, J F Mouscadet, P Cotelle

Affiliation

¹ Laboratoire de Chimie Organique Physique, UPRESA CNRS 8009, Université des Sciences et Technologies de Lille, Villeneuve d'Ascq, France.

PMID: 11720868
DOI: 10.1016/s0960-894x(01)00658-8

Abstract

Fourteen catechol and bis-catechol derivatives have been synthesised and tested for their HIV-1 inhibitory activities. The six more active molecules have been tested for their antiviral activity and cytotoxicity. We have found that bis-catechols 1 and 2 are the most active HIV-1 integrase inhibitor whereas the best antiviral compound is 4.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Catechols / chemical synthesis*
Catechols / pharmacology*
Cell Line
HIV Integrase Inhibitors / chemical synthesis*
HIV Integrase Inhibitors / pharmacology*
HIV-1 / drug effects
HIV-1 / enzymology
Humans
Magnetic Resonance Spectroscopy
Microbial Sensitivity Tests
Virus Replication / drug effects

Substances

Catechols
HIV Integrase Inhibitors