Aromatic ketones and uses thereof.
OHSU # 1004
Researchers at OHSU and Portland's VA Medical Center have discovered a series of chemical compounds, namely naphthoquinones, anthraquinones, and anthrones, that contain a unique and defining structural element making them selectively potent antiparasitic agents.
These new compounds exhibit an improvement in antimalarial potency of over 50 fold (as compared with currently used therapeutics) against most multidrug resistant strains of the malarial parasite. The new compounds act by a different mechanism than commercially available compounds against strains of the parasite that are resistant to a multiplicity of standard antimalarial drugs. Laboratory tests show these new compounds are at least 10 times more potent than chloroquine and 100 times more active than quinine, the standard drugs used to treat malaria in humans.
These results suggest their use in treating both the liver and blood stages of malaria. Therefore it is reasonable to assume that the compounds may be of use as prophylactic agents used to prevent the disease.
The obvious advantages of this technology are its potential use as a new remedy for malaria. Of the parasitic agents causing disease in humans, malaria is the single most destructive and dangerous infectious agent in the developing, chiefly tropical, world. Malaria infects half a billion, causes serious disease in 100-200 million, and kills roughly 2 million people every year. Safe and effective anti-malarial agents are urgently needed, even against multi-drug resistant strains of the malarial parasite.
Currently, experiments are underway in the laboratory to synthesize additional representative compounds, as well as antimalarial testing in vitro and in vivo in malaria-infected animals.
- Michael Riscoe, SM.Molecular Microbiology & Immunology
- Rolf Winter
- Jane Kelly
- Martin Smilkstein
- David Hinrichs
For more information, contact:
Senior Technology Development Manager