Application of compound (E)-N-[2-(3,4-dimethoxyphenyl)ethyl]-3-phenylacrylamide in preparation for medicine resisting Alzheimer disease

Abstract

The invention provides an application of (E)-N-[2-(3,4-dimethoxyphenyl)ethyl]-3-phenylacrylamide compound 1 in preparation for a medicine resisting Alzheimer disease. An animal experiment for the nerve cells of a primary SD rat displays that: the compound 1 can be bound with alpha7nAChR, and the binding site is as the same as the binding site of bungatotoxin. Anti-inflammatory activity experiment prompts that the compound 1 has good anti-inflammatory activity. The compound 1 remarkably improves the toxicity of the nerve cells of the primary SD rat, and has a neuroprotective effect. Moreover, the compound 1 can directly act on amyloid protein, so as to achieve reduction for the toxic effect on the nerve cells acted by beta-amyloid. An experiment of treating a mouse by scopolamine indicates that the compound 1 can effectively improve the learning ability and the memory ability of experimental animal. The experiment shows that the compound 1 can effectively treat the senile dementia induced by beta-amyloid by means of exciting alpha7-acetylcholine receptor, depolymerizing beta-amyloid and the like. Therefore, the compound 1 can be used for preparing a medicine resisting Alzheimer disease, and has great clinical application value.

Description

technical field The present invention relates to medicines, in particular to anti-Alzheimer's disease medicines, especially compound (E)-N-[2-(3,4-dimethoxyphenyl)ethyl]-3-phenylacrylamide ( gx50) in the preparation of anti-Alzheimer's disease drugs. Background technique Alzheimer's disease, also known as senile dementia, is a neurodegenerative disease. The main clinical manifestation is that there are obstacles in memory, thinking, analysis and judgment, visuospatial recognition, emotion, etc. in the state of no disturbance of consciousness. The patient's memory ability gradually declines. The accumulation of Aβ-amyloid (β-amyloid) in the brain is an important pathological feature of Alzheimer's disease. Aβ-amyloid (β-amyloid) can poison neurons, leading to the apoptosis of neurons. Current anti-Alzheimer's drugs focus on preventing the amyloid-beta (Aβ) peptide from poisoning neuronal cells. Including 1), designing small molecules or polypeptides to competitively bind ...

AI Technical Summary

Problems solved by technology

Amyloid-beta (Aβ) peptides are toxic to cholinergic receptors, rendering these ion channels (such as α7nAChR) unable to carry out their signaling role