Butyrylcholine esterase selective inhibitor as well as preparation method and application thereof

A technology for butyrylcholinesterase and butyrylcholine, which is applied in the field of butyrylcholinesterase selective inhibitors and its preparation, can solve the problems of lack of structural novelty, poor diversity selectivity, and small quantity , to achieve good in vitro activity
CN112979546AActive Publication Date: 2021-06-18CHINA PHARM UNIV
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Patent Information

Authority / Receiving Office
CN ยท China
Patent Type
Applications(China)
Current Assignee / Owner
CHINA PHARM UNIV
Publication Date
2021-06-18

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Abstract

The invention discloses a butyrylcholine esterase selective inhibitor as well as a preparation method and application thereof. The inhibitor is a compound shown as a formula (I). The invention also discloses application of the compound in preparation of drugs for preventing or treating Alzheimer's disease. Experiments such as butyrylcholine esterase inhibitory activity, selective screening, Nrf2 activation activity, Morris water maze and the like are used as carriers to evaluate the treatment of Alzheimer's disease (especially moderate and severe Alzheimer's disease) by the compound shown in the formula (I), and the compound is found to have good in-vitro and in-vivo activity and extremely high selectivity. The compound can be used as a precursor substance for further development of Alzheimer's disease by selectively inhibiting butyrylcholine esterase.
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Description

technical field

[0001] The invention relates to a class of butyrylcholinesterase inhibitors and their preparation methods and uses, in particular to a class of butyrylcholinesterase selective inhibitors and their preparation methods and uses. Background technique

[0002] Alzheimer's disease (AD) is a systemic brain neurodegenerative syndrome with a slow course, difficult to detect and irreversible. Clinical manifestations include central cognitive impairment, mental and motor disturbances, etc. Since the incidence of AD will increase with age, in today's society where population aging is getting worse, AD has posed a huge threat to the life and health of the elderly and the overall medical resources of the society, and has become a global medical problem. . According to the "2019 World Alzheimer's Disease Report" statistics, in 2019, there were more than 50 million AD patients worldwide, and by 2050, this number is expected to reach 152 million, which is equivalent to 1 p...

Claims

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