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Carboline compounds, and synthetic method and anti-acetylcholinesterase activity thereof

A synthesis method and compound technology, which are applied in the fields of carboline compounds and their synthesis, and anti-acetylcholinesterase activity, can solve the problems that have not yet been seen, and achieve the effect of strong inhibitory activity.

Active Publication Date: 2017-04-26
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far, there have been no research reports on the anti-acetylcholinesterase and butyrylcholinesterase activities of 2-arylcarboline salts and 2-aryl-3,4-dihydrocarboline salts

Method used

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  • Carboline compounds, and synthetic method and anti-acetylcholinesterase activity thereof
  • Carboline compounds, and synthetic method and anti-acetylcholinesterase activity thereof
  • Carboline compounds, and synthetic method and anti-acetylcholinesterase activity thereof

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Embodiment Construction

[0047] The present invention will be described in detail below in combination with specific embodiments.

[0048] According to the structural characteristics, the carboline compounds involved in the present invention can be divided into A, B, C, and D types, wherein B and D types are 2-aryl carboline salt compounds, and A and C types are 2-aryl -3,4-Dihydrocarboline salt compound. The activity test shows that the compound involved in the present invention has significant inhibitory activity on AChE and BChE, and has great potential as an active ingredient for preparing a drug for treating AD.

[0049] The carboline compound has the following molecular structure:

[0050] Class A:

[0051]

[0052] Class B:

[0053]

[0054] Class C:

[0055]

[0056] Class D:

[0057]

[0058] in:

[0059] R 1 It is a hydrogen atom, an alkyl group, a cycloalkyl group, an unsaturated hydrocarbon group, an aryl group or an aromatic heterocyclic group, a heterocyclic hydrocarbo...

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Abstract

The invention relates to carboline compounds, and a synthetic method and anti-acetylcholinesterase activity thereof. The carboline compounds have been proved to have a plurality of biological activities like anti-microbe activity, anticancer and anti-virus activity; however, researches on the anti-acetylcholinesterase activity and anti-cholinesterase activity have not been reported in the prior art. The carboline compounds provided by the invention are classified into a class A, a class B, a class C and a class D, wherein the class B and the class D are 2-aryl carboline salt compounds while the class A and the class C are 2-aryl-3,4-dihydrocarboline salt compounds. Results of activity determination show that the compounds provided by the invention have substantial anti-acetylcholinesterase and anti-cholinesterase activities and have great potential as active ingredients for preparation of drugs used for treating the Alzheimer disease.

Description

technical field [0001] The invention relates to a class of compounds and applications thereof, in particular to a class of carboline compounds, their synthesis method and anti-acetylcholinesterase activity. Background technique [0002] Acetylcholine Esterase (AChE) is a serine hydrolase that is necessary for normal nerve conduction in the body. The main physiological function of AChE is to hydrolyze acetylcholine (ACh) in the cholinergic synaptic cleft into acetic acid and choline, thereby terminating the transmission of nerve impulses. AChE has strong catalytic performance and high specificity for acetylcholine at physiological concentrations. [0003] Alzheimer's disease (AD) is an age-related irreversible neurodegenerative disease characterized by progressive loss of memory, language function decline and other cognitive impairments. It is estimated that there are more than 40 million people suffering from AD in the world. Therefore, the harm of AD disease to public he...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/437A61P25/28
Inventor 周乐周搏航张冰玉崔志明候哲耿会玲
Owner NORTHWEST A & F UNIV
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