ANTIMALARIAL NAPHTHYLISOQUINOLINE ALKALOIDS AND PHARMACEUTICAL COMPOSITIONS AND MEDICAL USES THEREOF
The subject technology are novel naphthylisoquinoline alkaloid compounds, and methods of total synthesis thereof. Representative examples of these compounds have been shown to have potent in vitro activity against malaria parasites, including parasites that are highly resistant to available antimalarial drugs. Representative examples have also been shown to have potent in vivo activity against malaria parasites in animal models. Pharmaceutical compositions comprising these compounds, as well as methods of using the compounds to treat or prevent a malarial infection of a host, are claimed. The relative structural simplicity of this class of compounds, and the ready synthetic access thereto, provide unprecedented opportunities for structure-activity relationship (SAR), lead-optimization and antimalarial drug development.
Granted Patent Reference Number(s): PCT, Application No. PCT/US95/01717, Filed 13 Feb 1995"; US, , Patent No. 5,639,761, Issued 17 June 1997; HHS Reference No. E-090-1994/0-PCT-02; "HHS, Reference No. E-090-1994/0-US-01