A kind of pyronaridine compound and its application

A kind of pyronaridine and compound technology, applied in the field of antimalarial pyronaridine compounds
CN103570711BInactive Publication Date: 2016-08-03SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Publication Date
2016-08-03
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides pyronaridine compounds and applications thereof. The general formula of the pyronaridine compounds is shown as the formula I, wherein R1, R2, R3, and R4 are acting sites, and therefore the compounds have activity of inhibiting plasmodium in-vivo PDE. The pyronaridine compounds have a binding free energy lower than pyronaridine, and therefore the pyronaridine compounds have higher activity of inhibiting the plasmodium in-vivo PDE than the pyronaridine, and therefore the pyronaridine compounds have stronger anti-malarial activity.
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Description

technical field

[0001] The present invention relates to a pyronaridine compound and its use, in particular to a pyronaridine structure optimization to make it have lower binding free energy and higher inhibition of PDE (phosphodiesterase) in Plasmodium. ) active antimalarial pyronaridines. Background technique

[0002] Pyronaridine (PYR) is a Plasmodium erythrocytic anamorphic agent created in my country in 1970, code-named 7351. The chemical name of the corresponding drug is 2-methoxy-7-chloro-10-[3′,5′-bis(pyrrolidinyl-1-methyl)-4′-hydroxy-phenyl]aminobenzo[ b] 1,5-naphthyridine tetraphosphate, the trade name is malaridine, and the molecular formula is:

[0003]

[0004] PYR can effectively act on Plasmodium falciparum. The order of sensitivity to pyronaridine at different developmental stages of the red inner stage protozoa is ring body > trophozoite > schizont, and the effect on pyronaridine is greater than that of chloroquine on all stages of protozoa. [00...

Claims

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