Conjugated product of dihydroartemisinin and quinolones, preparation method and application thereof

A technology of dihydroartemisinin and quinolones, which is applied in the field of chemistry, can solve the problems of low bioavailability and fast excretion from the body, and achieves the effect of a simple preparation method
CN104418864BActive Publication Date: 2016-06-08SOUTHWEST UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SOUTHWEST UNIV
Publication Date
2016-06-08

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Abstract

The invention discloses conjugates of dihydroartemisinin and quinolones compounds shown in formulae I to IV and officinal salt thereof, wherein X is -CH2CH2-, -CH2CH2CH2- or -COCH2CH2CO-. The conjugates have a certain antibacterial effect on a mycobacterium tuberculosis standard sensitive strain, a clinical separating sensitive strain and a clinical separating drug resistance strain, and especially the inhibitory effects of conjugates of dihydroartemisinin and clinafloxacin on the mycobacterium tuberculosis standard sensitive strain, the clinical separating sensitive strain and part of the clinical separating drug resistance strain are stronger than those of independent dihydroartemisinin and clinafloxacin. The conjugates can be used for preparing antituberculosis drugs and have a potential application prospect in tuberculosis prevention and cure field. The formulae I to IV are as shown in the specification.
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Description

technical field

[0001] The invention belongs to the field of chemistry, relates to a conjugate prepared by coupling two drugs, and also relates to a preparation method of the conjugate and its application in the field of pharmacy. Background technique

[0002] Artemisinin was discovered by Tu Youyou from the plant Artemisia annua according to the description of ancient Chinese medical scientists. Artemisinin was initially used in clinical treatment as a class of antimalarial drugs with a new structure, which showed unique therapeutic effects, but it was accompanied by the disadvantages of low bioavailability and rapid excretion in the body. To overcome this problem, scientists derivatized its structure and synthesized the first generation of artemisinin derivatives. Representative molecules include dihydroartemisinin (DHA), artemether, artether and artesunate . This type of molecule shows more excellent pharmaceutical properties. Among them, dihydroartemisinin, artemether ...

Claims

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