The total synthesis of fukiic acid, an HIV-1 integrase inhibitor

Clémence Queffélec; Fabrice Bailly; Gladys Mbemba; Jean-François Mouscadet; Zeger Debyser; Myriam Witvrouw; Philippe Cotelle

doi:10.1016/j.ejmech.2007.12.013

The total synthesis of fukiic acid, an HIV-1 integrase inhibitor

Eur J Med Chem. 2008 Oct;43(10):2268-71. doi: 10.1016/j.ejmech.2007.12.013. Epub 2007 Dec 27.

Authors

Clémence Queffélec¹, Fabrice Bailly, Gladys Mbemba, Jean-François Mouscadet, Zeger Debyser, Myriam Witvrouw, Philippe Cotelle

Affiliation

¹ Laboratoire de Chimie Organique et Macromoléculaire, CNRS UMR 8009, Université de Lille 1, 59655 Villeneuve d'Ascq, France.

PMID: 18243421
DOI: 10.1016/j.ejmech.2007.12.013

Abstract

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.

Publication types

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

MeSH terms

Animals
Base Sequence
Cattle
Cell Line
HIV Integrase / metabolism*
HIV Integrase Inhibitors / chemical synthesis*
HIV Integrase Inhibitors / chemistry
HIV Integrase Inhibitors / pharmacology*
Humans
Phenylpropionates / chemical synthesis*
Phenylpropionates / chemistry
Phenylpropionates / pharmacology*
Succinates / chemical synthesis*
Succinates / chemistry
Succinates / pharmacology*

Substances

HIV Integrase Inhibitors
Phenylpropionates
Succinates
fukiic acid
HIV Integrase
p31 integrase protein, Human immunodeficiency virus 1