Dihydroartemisinin-containing carboxy phenol/ester phenol/amido phenol conjugate as well as synthesis method and application thereof

A technology of amidophenol conjugates and dihydroartemisinin, which is applied in the field of chemical medicine, can solve the problems of insufficient system and small number of compounds, and achieve the effect of simple synthesis method, high synthesis yield and good application prospect
CN110590804AActive Publication Date: 2019-12-20SOUTHWEST UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SOUTHWEST UNIVERSITY
Publication Date
2019-12-20

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Abstract

The invention discloses a dihydroartemisinin-containing carboxy phenol / ester phenol / amido phenol conjugate. The conjugate or a racemate, stereoisomer and tautomer thereof and a pharmaceutically acceptable salt of the conjugate have a structural general formula as shown in a formula I, wherein n is equal to 2 or 3, X is an alkoxyl, a hydroxyl, an amino group or -O(CH2)b-DHA, Y is -H or an alkoxyl,Z is an alkenyl and an alkyl or has no groups, b is equal to 2 or 3, and DHA represents for dihydroartemisinin. The invention further discloses a synthesis method of the dihydroartemisinin-containingcarboxy phenol / ester phenol / amido phenol conjugate and an application of the conjugate as a drug for resisting to tuberculosis and diabetes mellitus, reducing blood fat and inhibiting interleukin-17.
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Description

technical field

[0001] The invention relates to the technical field of chemistry and medicine, in particular to a dihydroartemisinin-containing carboxyl phenol / ester phenol / amide phenol conjugate, a synthesis method and an application. Background technique

[0002] Artemisinin is a terpenoid compound found in the plant Artemisia annua, which is a colorless needle-like crystal. Dihydroartemisinin (DHA) is the first-generation derivative of artemisinin. It not only has a unique structure, but also shows better pharmaceutical properties than artemisinin. It is an important clinical antimalarial drug. Based on the special structure and excellent activity of DHA, the research on DHA continues. At present, it mainly focuses on the design and synthesis of new derivatives of DHA, and the exploration of new activities of old molecules or new molecules of DHA. So far, many new derivatives of DHA have been synthesized, and some artemisinin derivatives have been used in clinical trials...

Claims

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