Qinghaosu derivatives

Classen, W., Altmann, B., Gretener, P., Souppart, C., Skelton-Stroud, P. and Krinke, G. (1999) Differential effects of orally versus parenterally administered qinghaosu derivative artemether in dogs. Experimental and Toxicologic Pathology, 51, 507-516. 

Microbial transformation study can serve as a model for the study of qinghaosu metabolism in the mammalian and can unshed the new pathway to qinghaosu derivatives. Therefore, several research groups have endeavored to transform qinghaosu with different microbes and have found that the hydroxy group can be introduced in some inactive carbon positions of qinghaosu. 

When artemether and sodium artesunate were successfully used by intramuscular or intravenous administration for treatment of severe malarial patients, their shortcomings, such as short half-life and instability of aqueous solution of sodium artesunate, were cognized. Hence, qinghaosu derivatives and analogs numbering in the thousands were synthesized and evaluated by many research groups worldwide. 

Sodium artesunate is the first water-soluble qinghaosu derivative and used for treatment of the severe malaria patients by intravenous or intramuscular administration. However, the aqueous solution is unstable, and its hydrolysis product,... 

In view of the known basic antimalarial drugs (such as chloroquine, quinine) that are being used as salts for injection, it was proposed that introducing an amino group into the qinghaosu molecule may lead to water-soluble derivatives. Thus, five types of basic qinghaosu derivatives were synthesized (Structure... 

Some research groups synthesized steroidal qinghaosu derivatives in which the qinghaosu nucleus, trioxane, or tetraoxane combined with a steroidal skeleton in... 

Since then, several qinghaosu derivatives have been treated with ferrous sulfate in the same reaction condition. Except for some hydrolysis products, similar derivatives of tetrahydrofuran compound 28 and 3-hydroxy deoxyqinghaosu 15 were... 

Tang, Y., Jiang, H.L., Chen, K.X. and Ji, R.Y. (1996). QSAR Study of Artemisinin (Qinghaosu) Derivatives Using Neural Network Method. Indian J. Cherrt, 35B, 325-332. 

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