Water-soluble arteannuin derivative and preparation method thereof

A water-soluble technology of artemisinin derivatives, applied in pharmaceutical formulations, drug combinations, allergic diseases, etc., can solve the problems of low oral bioavailability, short half-life, damage to the central nervous system, etc., to increase bioavailability , reduce toxic and side effects, and have novel synthetic ideas
CN101293889AInactive Publication Date: 2008-10-29CHONGQING UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
CHONGQING UNIV
Publication Date
2008-10-29
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a water-soluble arteannuin derivative and a preparation method thereof. The method comprises the following steps of: (1) preparing dihydroarteannuin; (2) preparing tetra-acetyl-mannopyranosyl bromide; and (3) preparing the water-soluble arteannuin derivative. The water-soluble arteannuin derivative is proven to have good water solubility, is easy for preparing preparations and has good pharmaceutical prospect after structural identification and water solubility analysis. The inventive preparation method has the advantages of simple operation, mild reaction conditions, and no need of deprotection step. After initial cell experiments, the water-soluble arteannuin derivative is proven to have no toxic or side effects on normal cells.
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Description

technical field

[0001] The invention belongs to the field of chemical pharmaceutical engineering, and specifically relates to a water-soluble artemisinin derivative and its preparation and application. Background technique

[0002] Artemisinin (artemisinin) is a new type of antimalarial drug extracted from Artemisia annua L. by Chinese scientists in 1971. It has the characteristics of high efficiency, quick action and low toxicity. It is the only one recognized by the World Health Organization in China. The botanical medicine researched and developed according to the research standard of western medicine is also the first traditional Chinese medicine product that is truly recognized globally. However, artemisinin's poor solubility and high recurrence rate limit its clinical application. Medicinal chemists began to do a lot of research on the structure modification and structure-activity relationship of artemisinin, and screened out some drugs with better curative effect. Th...

Claims

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