Novel stilbene derivative and preparation method thereof

Abstract

The invention provides a novel stilbene derivative. The novel stilbene derivative is a compound with a general formula I or II as described in the specification or a salt formed by the compound with the general formula I or II as described in the specification and inorganic acid or organic acid. In the general formula I or II, X represents a hydrogen atom or halogen atom; R represents a substituent selected from a group consisting of C1-5 alkyl groups, C2-4 alkenyl groups, C2-4 alkynyl groups, C3-6 cycloalkyl groups, five-to-twelve-component aryl groups, two-to-five-component heteralkyl groups, three-to-six-component hetercycloalkyl groups, five-to-twelve-component heteraryl groups, substituted three-to-six-component cycloalkanes, substituted five-to-twelve-component aryl groups and substituted five-to-twelve-component heteralkyl groups; or the substituent represented by R is a first substituent formed by a spacer group and any one selected from a group consisting of C3-6 cycloalkanes, three-to-six-component hetercycloalkanes, five-to-twelve-component aryl groups and five-to-twelve-component heteraryl groups, and the spacer group comprises -CH2-, -(CH2)2-, -CH=CH-, -CH2O-, -CH(OCH3)- and -CH2S-.

Description

technical field [0001] The invention relates to the fields of chemical synthesis and pharmacy, in particular to a novel stilbene derivative and a method for preparing the novel stilbene derivative. Background technique [0002] Alzheimer's disease (Alzheimer's disease, AD) is a degenerative disease of the central nervous system. In the early stage, it is a hidden cognitive decline, which develops into severe memory loss, behavior and personality changes, language barriers, loss of Ability to live independently. In 2015, the number of registered cases worldwide reached 46.8 million, and it was listed as the fourth leading cause of death after cardiovascular disease, stroke and tumors. So far, there is no drug that can reverse or stop the development of the disease. [0003] The basic pathological changes in the brain of AD patients include amyloid plaques, neurofibrillary tangles, and neuronal loss. A large number of animal experiments have proved that in the subventricular...

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Problems solved by technology

[0005] However, there are still several important problems to be solved in the current research on neurogenesis: 1) most of the research is random trial and error screening, and the report of structure-activity relationship research is very scarce, which is not conducive to the rational design and screening of more active compounds; 2) ) Most of the research is screening for new indications of compounds with other pharmacological activities, so these pharmacological side effects will limit its clinical application prospects in the treatment of dementia, for example, other pharmacological activities of resveratrol damage the hippocampus of adult healthy rats 3) The blood-brain barrier is an important obstacle for neuropharmaceuticals. Many drugs do not meet the optimal physical and chemical properties of breaking through the lipophilic blood-brain barrier. For example, too many hydrogen bond donors will lead to low permeability, and eventually manifest When the dosage is very large (for example, the intraperitoneal injection dosage of resveratrol with three phenolic hydroxyl groups is 40 mg / Kg to observe the phenomenon of promoting neurogenesis in aged mice), which will inevitably limit the future clinical application. transform

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