Preparation method and application of tacrine-sinapic acid heterozygote

A technology of sinapinic acid and tacrine, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as limiting clinical application, and achieve strong inhibitory effect and obvious anti-oxidation activity, significant in vitro neuroprotective activity
CN107652233AActive Publication Date: 2018-02-02天津海润家和创新医药研究有限责任公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
天津海润家和创新医药研究有限责任公司
Publication Date
2018-02-02

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Abstract

The invention discloses a tacrine-sinapic acid heterozygote, a medicinal composition containing the tacrine-sinapic acid heterozygote, and a preparation method and application thereof. The tacrine-sinapic acid heterozygote has the following structure: the formula is as shown in the description. Experiments prove that the tacrine-sinapic acid heterozygote has high inhibitory activity on acetylcholin esterase (AChE) and butyrylcholine esterase (BuChE), has acetylcholin esterase inhibition capability which is 15 times that of tacrine, has strong inhibition effect on amyloid protein (Abeta) self-aggregation, has remarkable anti-oxidation activity, does not have remarkable in-vitro neurocytotoxicity and in-vivo acute hepatotoxicity, shows remarkable in-vitro nerve cell protective activity, andcan be applied to treatment on Alzheimer's disease.
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Description

technical field

[0001] The invention belongs to the field of organic synthesis and medicine, and in particular relates to a tacrine-sinapinic acid hybrid for treating Alzheimer's disease, a pharmaceutical composition containing the tacrine-sinapinic acid hybrid, a preparation method and an application thereof , especially relates to the preparation of tacrine-sinapinic acid hybrid by reacting aminotacrine with sinapinic acid, and the application of the tacrine-sinapinic acid hybrid in the preparation of anti-Alzheimer drugs. Background technique

[0002] Tacrine is the first drug approved by the FDA for the treatment of Alzheimer's disease (AD), which belongs to the first generation of acetylcholinesterase inhibitors. However, its clinical application is limited due to severe liver toxicity. Studies have confirmed that the hepatotoxicity of tacrine is closely related to its free primary amino groups. Current studies mostly use molecular fragments with different functions to...

Claims

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