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Antiparasitic Artemisinin Derivatives (Endoperoxides)

总结

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.

技术优势

1. Compound are relatively accessible by conducting straight forward chemical transformation on starting materials that are commercially available in large quantities
2. Families of compounds can be prepared
3. Structural variation of the compounds can be achieved in control
4. Reduced neotoxicity
5. More stable
6. Solve multidrug resistant strains found in antimalarial drugs for agricultural animal

技术应用

- Provides a wide range of new drugs against malaria and related parasitic infections in farm animals, including neosporosis and coccidiosis

附加资料

Patent Number: US9043927B2
Application Number: US13769846A
Inventor: Hu, Haibo | Xu, Jianliang | Chen, Qian
Priority Date: 27 Sep 2012
Priority Number: US9043927B2
Application Date: 19 Feb 2013
Publication Date: 26 May 2015
IPC Current: H04L002906 | H04W001206
US Class: 726026 | 726027 | 726030
Assignee Applicant: Neo Mechanic Limited | Hong Kong Baptist University
Title: Method and apparatus for authenticating location-based services without compromising location privacy
Usefulness: Method and apparatus for authenticating location-based services without compromising location privacy
Summary: Computer processor implemented method for privacy-preserving query authentication.
Novelty: Computer processor implemented method for privacy-preserving query authentication, involves storing unconditional location privacy, when authenticating queries such that client cannot infer any information about locations of users

主要类别

生物医学

细分类别

医药成分

申请日期

31 Jul 2001

申请号码

US 09/743827

专利信息

US 6984640

ID号码

TTC.PA.072

国家/地区

香港