title: Synthesis and HIV-1 integrase inhibitory activities of catechol and bis-catechol derivatives.
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.
authors.affiliation: Laboratoire de Chimie Organique Physique, UPRESA CNRS 8009, Université des Sciences et Technologies de Lille, Villeneuve d'Ascq, France.
authors.forename: R
authors.initials: R
authors.lastname: Dupont
authors.forename: L
authors.initials: L
authors.lastname: Jeanson
authors.forename: J F
authors.initials: JF
authors.lastname: Mouscadet
authors.forename: P
authors.initials: P
authors.lastname: Cotelle
mesh_terms: D002396:Catechols / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D014779:Virus Replication / Q000187:drug effects
chemical_list: D002396:Catechols; D019428:HIV Integrase Inhibitors