A kind of stilbene derivative and preparation method thereof

Abstract

The present invention provides a novel stilbene derivative, the novel stilbene derivative is a compound having the following general formula I or II, or the novel stilbene derivative has the An acceptable salt formed by the compound of the general formula I or the general formula II and an inorganic acid or an organic acid; Wherein, in the general formula I or the general formula II, the atom represented by X is a hydrogen atom or a halogen atom; the substituent represented by R is C1-C6 alkyl, 1-6-membered heteroalkyl, C2-C4 alkene Base, C2‑C4 alkynyl, C3‑C6 cycloalkyl, substituted C3‑C6 cycloalkyl, 3‑6 membered heterocycloalkyl, substituted 3‑6 membered heterocycloalkyl, 5‑18 membered aryl, substituted 5-18-membered aryl group, 5-18-membered heteroaryl group, substituted 5-18-membered heteroaryl group; the novel stilbene derivatives have neurogenesis activity and low neurocytotoxicity.

Description

technical field [0001] The invention relates to the fields of chemical synthesis and pharmacy, in particular to a novel stilbene derivative and a preparation method of the novel stilbene derivative. Background technique [0002] Alzheimer's disease (AD) is a degenerative disease of the central nervous system that begins with latent cognitive decline and develops into severe memory loss, behavioral and personality changes, language impairment, loss of independent living ability. 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 cancer, and there was no clinical cure. The incidence of Alzheimer's disease is closely related to age. With the increase of age, the incidence of AD increases exponentially. According to statistics, the incidence of AD is about 1% at the age of 60, and then averages every 5- In 6 years, the incidence doubles. With the intensificatio...

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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 studies are random trial and error screening, and few reports with common groups (especially pharmacophore) are involved, which is not conducive to further strengthening Design and screening of active compounds; 2) Most of the research is based on the screening of other known targets or compounds with other pharmacological activities, so these pharmacological side effects will limit its clinical application prospects in the treatment of dementia; 3) Blood-brain The barrier is an important obstacle for neurological drugs. Many drugs do not meet the optimal physical and chemical properties to break through the blood-brain barrier. The brain barrier is finally reflected in a very large dosage (for example, the intraperitoneal injection dosage of resveratrol with three phenolic hydroxyl groups is 40mg / Kg), which will inevitably limit future clinical applications, and structural modification is necessary

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