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Antiparasitic artemisinin derivatives (Endoperoxides)

Authors Haynes, Richard Kingston HKUST affiliated (currently or previously)
Chan, Ho-Wai HKUST affiliated (currently or previously)
Lam, Wai-Lun
Tsang, Hing-Wo HKUST affiliated (currently or previously)
Cheung, Man-Ki
Voeste, Arnd
Schmuck, Gabriele
Greif, Gisela
Issue Date 2007-12-10
Source Vietnam Patent , for Invention No. 6741
Summary New antiparasitic qinghaosu derivatives are discovered. The new derivatives of qinghaosu (QHS, or artemisinin) and synthetic trioxane are more active, more stable, and more bioavailable than qinghaosu itself and its current commercially available derivatives.These new derivatives involve alteration of the qinghaosu molecule such that a known decomposition pathway is now no longer available. In addition, certain of the groups attached, specifically amino groups, render the derivatives water soluble, and hence facilitate administration and absorption. Neurotoxicity, one of the biggest potential problems with current derivatives, is also reduced by removing the oxygen atom at C-10. Tests conducted on the derivatives shown that antimalarial activities of several C-10 amino and aryl derivatives are equipotent to, or more potent than, those of artemisinin and dihydroartemisnin, and the C-16 derivatives are less potent. Derivatives have also been tested against Neospora caninum at Bayer Leverkusen and activities have been rated as good against control compounds. Malaria is the world!\s most prevalent parasitic disease in humans at the moment. Whilst the current qinghaosu derivatives are successful, there are problems associated with stability, bioavailability, and potential neurotoxicity. Besides, the demand for new qinghaosu-based drugs for animal health against parasitemia functionally related to malaria, and for improved antimalarial drugs for agricultural animals against parasitic diseases, revealed that there are great needs for new antiparasitic qinghaosu derivatives.
Language English
Format Patent