The total synthesis of fukiic acid, an HIV-1 integrase inhibitor.
A successful synthesis of fukiic acid is described in 7% overall yield (6 steps from veratraldehyde). rac-Fukiic acid was found to be a potent inhibitor of HIV-1 integrase but did not reveal any antiviral activity in the MT-4 cells assay.
Queffélec
Clémence
C
Laboratoire de Chimie Organique et Macromoléculaire, CNRS UMR 8009, Université de Lille 1, 59655 Villeneuve d'Ascq, France.
Bailly
Fabrice
F
Mbemba
Gladys
G
Mouscadet
Jean-François
JF
Debyser
Zeger
Z
Witvrouw
Myriam
M
Cotelle
Philippe
P
D000818:Animals; D001483:Base Sequence; D002417:Cattle; D002460:Cell Line; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013386:Succinates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D019428:HIV Integrase Inhibitors; D010666:Phenylpropionates; D013386:Succinates; C116091:fukiic acid; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1