2-Hydroxychalcone amine compound, its preparation method and use

Abstract

The invention discloses 2-hydroxychalcone amine compounds and pharmaceutically-acceptable salts, preparation method thereof, pharmaceutical composition, and uses for preparing medicines treating and / or preventing neurodegenerative related diseases, the diseases including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntingdon's disease, HIV associated dementia, multiple sclerosis, progressive lateral sclerosis, neuropathic pain, glaucoma and other neurodegenerative diseases.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to a novel 2-hydroxychalcone amine compound (I) and a pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition and a preparation method for treating and / or preventing neurodegeneration Sex-related diseases, including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, progressive lateral sclerosis, neurological Pain, glaucoma and other neurodegenerative diseases. Background technique [0002] Alzheimer's disease (Alzheimer's disease, AD, senile dementia) is a degenerative disease of the central nervous system mainly characterized by progressive cognitive impairment and memory impairment. Vascular diseases and cancers are high-incidence diseases, which have risen to the fourth cause of death in developed countries such as Europe and the United States. Accor...

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Problems solved by technology

In the previous research, we designed and synthesized scutellarin aglycon carbamate derivatives (CN101337956A, CN102603698A), stilbene or ethane carbamate for the acetylcholinesterase and oxidative stress factors in the pathogenesis of AD Ester compounds (CN102816090A), isoflavone carbamate compounds (CN102827131A), flavonoid alkylamine compounds (CN103087024A), genistein alkylamine compounds (CN103113340A), stilbene oxyalkylamine compounds (CN103073440A), although these compounds have good acetylcholinesterase inhibitory and antioxidant activities, but for A β 1-42 Inhibition of self-aggregation (inhibition rates of less than 65.0% at 20.0 µM concentration), Cu 2+ Induced A β 1-42 Inhibition of aggregation (inhibition rates of less than 65.0% at a concentration of 20.0 µM) and 2+ Induced A β 1-42 The aggregation disaggregation activity (the disaggregation rate is less than 60.0% at the concentration of 20.0µM) is not satisfactory, resulting in the poor efficacy of these compounds on AD in animal models

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