Abstract
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.
Keywords: Molecular scaffold, HIV integrase inhibitors, styrylquinolines