5-Hydroxy-6-Quinaldic Acid as a Novel Molecular Scaffold for HIV-1 Integrase Inhibitors

Autor: Polanski, J., Niedbala, H., Musiol, R., Podeszwa, B., Tabak, D., Palka, A., Mencel, A., Finster, J., Mouscadet, J.- F., Bret, M. L.
Zdroj: Letters in Drug Design & Discovery; April 2006, Vol. 3 Issue: 3 p175-178, 4p
Abstrakt: 8-Hydroxy-7-quinaldic acid can be considered as a basic scaffold for all reported styrylquinoline HIV-1 integrase inhibitors. However, when tested in vitro, this compound appeared to be inactive against the enzyme. We have designed and synthesized an improved molecular fragment, i.e. 5-hydroxy-8-nitro-6-quinaldic acid, which appeared to inhibit HIV-1 integrase in vitro.
Databáze: Supplemental Index