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 general formula II shown as the specification, or is an acceptable salt formed by the compound with the general formula I or general formula II and an inorganic acid or organic acid. Specifically, in the general formula I or general formula II, the atom represented by X is hydrogen atom or halogen atom, the substituent group represented by R is C1-C6 alkyl, 1-6 membered heteroalkyl, C2-C4 alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl, substituent C3-C6 cycloalkyl, 3-6 membered heterocycloalkyl, substituent 3-6 membered heterocycloalkyl, 5-18 membered aryl, substituent 5-18 membered aryl, 5-18 membered heteroaryl, and substituent 5-18 membered heteroaryl. The novel stilbene derivative has neurogenesis activity and low nerve cell toxicity.

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 cases registered worldwide reached 46.8 million, and it was listed as the fourth leading cause of death after cardiovascular disease, stroke and tumor, and there is no clinical cure. The incidence of Alzheimer's disease is closely related to age. As the age increases, the incidence of AD increases exponentially. According to statistics, the incidence of AD is 1% at the age of 60, and thereafter every 5- In 6 years, the incidence rate will doub...

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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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