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Title: Antiparasitic artemisinin derivatives (Endoperoxides)
Other Titles: 抗寄生虫青蒿素衍生物,制备方法及組合物和用途
Authors: Haynes, Richard K.
Chan, Ho Wai (陳浩懷)
Lam, Wai-Lun (林威倫)
Tsang, Hing Wo (曾慶和)
Cheung, Man Ki (張文驥)
Voeste, Arnd
Schmuck, Gabriele
Greif, Gisela
Keywords: Drugs
Issue Date: 24-Sep-2003
Citation: 中國專利 ZL 99 8 10650.X
Abstract: 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.
Rights: This patent is also available at HKUST Technology Transfer Center Patent Search at <>
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