Tacrine-8-hydroxyl(amine)quinoline derivative and application thereof

A technology of tacrine and quinoline, applied in the field of biomedicine, can solve the problems of irreversible or curable diseases, high liver toxicity, and low bioavailability
CN105367553AInactive Publication Date: 2016-03-02GUANGDONG UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
GUANGDONG UNIV OF TECH
Publication Date
2016-03-02
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention relates a tacrine-8-hydroxyl(amine)quinoline derivative and applications thereof, and belongs to the technical field of biological medicines. The derivative comprises a compound of a formula I and a pharmaceutically acceptable salt thereof. A preparation method thereof comprises the step of: performing reductive amination and deprotection on the compounds Id and Ii and an intermediate In / In' to obtain a compound I, wherein the compound I can react in an alcohol solution to produce a salt. Pharmacological tests verify that the compound has the activity against Alzheimer's disease and can inhibit acetylcholinesterase and butyrylcholinesterase activity, and meanwhile can inhibit self-polymerization of the beta-amyloid protein, and has a certain chelating effect on metal ions, particularly Cu<2+> and Zn<2+>, so that the hydrolysis of the acetylcholinesterase and the self-polymerization of the beta-amyloid protein are retarded, the effect of the acetylcholinesterase on synapses is improved, and the metal ions in the brain is regulated, and therefore the compound is effective for treating Alzheimer's disease.
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Description

technical field

[0001] The invention relates to a tacrine-8-hydroxy(amino)quinoline derivative and its application, in particular to a tacrine-8-hydroxy(amino)quinoline derivative and its anti-Alzheimer The application in mutism drugs belongs to the technical field of biomedicine. Background technique

[0002] Alzheimer's disease (AD) is a neurodegenerative disease with insidious onset and progressive development. AD is characterized by a gradual decline in cognitive functions such as memory, thinking, comprehension, calculation, language, learning ability, and judgment. Dementia is diagnosed when it is reduced enough to affect the individual's daily life behavior. Those who develop before the age of 65 are called premature aging Dementia; those who develop after the age of 65 are called senile dementia, which is a disease caused by multiple factors. The exact cause is still not conclusively clarified. There is considerable evidence that several forms of AD have a heritable...

Claims

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