Preparation and application of bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative

A technology of dihydroartemisinin and phloroglucinol, which is applied in the field of biomedicine, can solve the problems of high toxicity and narrow therapeutic window, and achieve the effects of low cytotoxicity, simple synthesis and broad application prospects
CN114213435AActive Publication Date: 2022-03-22YUN BAI YAO ZHENG WU TECH SHANGHAI CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
YUN BAI YAO ZHENG WU TECH SHANGHAI CO LTD
Publication Date
2022-03-22

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Abstract

The invention discloses a bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative, the structural formula of the bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative is shown in the specification, and the invention also provides a preparation method of the bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative shown in the general formula (I). The invention also provides an application of the bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative of the general formula (I) in preparation of a medicine for treating autoimmune diseases. The compounds provided by the invention are novel compounds for treating autoimmune diseases, have low cytotoxicity, can significantly inhibit immune cell proliferation, effectively inhibit ear swelling induced by 2, 4-dinitrofluorobenzene and plantar swelling induced by sheep erythrocytes on an ear swelling model and a plantar swelling model of delayed hypersensitivity, and can be used for treating autoimmune diseases. The compound shows a good dose-effect relationship, and has a very wide application prospect as a medicine for treating autoimmune diseases.
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Description

technical field

[0001] The invention belongs to the field of biomedicine and relates to a phloroglucinol derivative, in particular to the preparation and application of a bis-(10-deoxydihydroartemisinin)-phloroglucinol derivative. Background technique

[0002] Artemisinin is an antimalarial drug extracted and discovered by Chinese scientists from Artemisia annua.L. in the 1970s. It is a class of sesquiterpene lactone compounds with a special peroxide bridge structure. , is also the first internationally recognized natural medicine discovered by China. However, artemisinin is difficult to absorb when taken orally, and its bioavailability is low, so it is difficult to make a suitable dosage form. Scientists have synthesized artemisinin derivatives such as artemether and artesunate with better antimalarial effects by modifying the structure of artemisinin. In addition to good antimalarial activity, a large number of studies in recent years have shown that some artemisinin der...

Claims

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