Water-Soluble Trioxanes as Potent and Safe Antimalarial Agents

Parasitic infections, particularly malaria, are a serious and widespread public health problem. New and better therapeutic agents are needed to fight these parasitic infections. The trioxane drug, artemisinin, is an active anti-malarial constituent of the herb Artemisia annua L., Compositae. Both artemisinin and a number of related synthetic organic endoperoxides have been shown to have anti-malarial activity; however, concerns exist regarding possible side effects, such as neurotoxicity, for these compounds. Dr. Posner and his colleagues have invented compounds and methods for treating parasitic infections such as malaria and cerebral toxoplasmic encephalitis. These compounds are novel biologically-active 3-substituted trioxanes. The C3 position is a substituted or unsubstituted alkyl or aryl group of 1-20, preferably 1-12, carbon atoms. The 3-substituted trioxanes have 50% inhibitory concentrations (IC50) as low as 30nM for Plasmodium falciparum, the causative agent of malaria, in human red blood cells. Description (Set) Proposed Use (Set) C3 substituted trioxanes may be useful in the treatment of parasitic infections, particularly malaria and cerebral toxoplasmic encephalitis. Patent (Set) 5,932,591; 6,136,847; 1205927C; HK1047047

Patents:
US 5,932,591

Inventor(s): Posner, Gary H.

Type of Offer: Licensing



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