Synthesis and HIV-1 integrase inhibitory activities of catechol and bis-catechol derivatives.
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.
Dupont
R
R
Laboratoire de Chimie Organique Physique, UPRESA CNRS 8009, Université des Sciences et Technologies de Lille, Villeneuve d'Ascq, France.
Jeanson
L
L
Mouscadet
J F
JF
Cotelle
P
P
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
D002396:Catechols; D019428:HIV Integrase Inhibitors