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Acetylcholine esterase inhibitor and applications thereof

An acetylcholinesterase and inhibitor technology, applied in the field of acetylcholinesterase inhibitors, can solve problems such as poor therapeutic effect of AChE inhibitors, and achieve the effect of obvious neuroprotective effect

Inactive Publication Date: 2019-05-03
UNIV OF JINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the therapeutic effects of these AChE inhibitors are not good, and they can only provide limited remission or stabilization of the disease at a specific stage of disease development and are accompanied by severe side effects.

Method used

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  • Acetylcholine esterase inhibitor and applications thereof
  • Acetylcholine esterase inhibitor and applications thereof
  • Acetylcholine esterase inhibitor and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 The influence of compound on AChE enzymatic activity

[0023] Acetylcholinesterase (AChE), thioacetylcholine iodide (ATC) as a substrate, and 5,5-dithiobis(2-nitrobenzoic acid) (DTNB) as a chromogenic reagent were purchased from Sigma. The determination of AChE inhibitory activity was carried out with reference to the method reported by Ellan et al. (Ellman, G. L. et al. Biochem. Pharmacol. 1961, 7, 88.). Add 40 μL of phosphate buffer (pH = 8.0) to each well of a 96-well plate, and then add 0.39, 0.78, 1.56, 3.125, 6.25, 12.5, 25, 50 and 100 μM of 10 μL of the test compound solution or blank control into Then add 10 μL of AChE to the corresponding air and incubate at 37°C for 5 min on a shaker. Add 20 μL of DTNB solution and incubate on a shaker at 37°C for 5 min, then add 10 μL of substrate ATC and incubate on a shaker at 37°C for 3 min, measure the absorbance at 412 nm with a microplate reader, and calculate Inhibition rate of test compound on AChE. ...

Embodiment 2

[0026] Example 2 Compounds on Aβ 1-42 Induced protective effect of SH-SY5Y nerve cell injury

[0027] SH-SY5Y was purchased from the National Cell Bank of the United States, and was routinely cultured in DMEM medium containing 10% fetal bovine serum in an incubator at 37°C and 5% CO2 saturated humidity. Take 2-2.5×10 5 Cells / mL were seeded in 96-well plates, and experiments were performed after 24 h of culture. Replace with fresh culture medium, and divide the cells into normal group, Aβ 1-42 Injury model group, test compound pretreatment group. Compounds of formulas I, II and III (10 μM) were added to the test compound treatment group, EGCG (tea polyphenols) was added to the EGCG positive control group, and no addition was made to the Aβ group and the normal group. After culturing for 2 h, Aβ at a final concentration of 10 μM was added to each group except the normal group 1-42 , continue to culture for 24h, add MTT (final concentration 0.5 mg / ml), after culture for 3 ho...

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Abstract

The invention discloses an acetylcholine esterase inhibitor, (N-(2-(1H-indole-3-yl)ethyl)-3-amino-6-methyl-5,6,7,8-tetrahydrothiophene [2,3-b][1,6]naphthyridin-2-carboxamide, and applications of the inhibitor in preparation of drugs for preventing and / or treating AChE-related diseases and drugs for preventing and / or treating diseases caused by Abeta-induced nerve damage. The compound provided by the invention can inhibit AChE and has a significant neuroprotective effect on the Abeta-induced nerve damage, and can be used for preparation of the drugs for preventing and / or treating related neurodegenerative diseases such as Alzheimer Disease (AD).

Description

technical field [0001] The present invention relates to a kind of acetylcholinesterase inhibitor and application thereof, ( N -(2-(1 H -indol-3-yl)ethyl)-3-amino-6-methyl-5,6,7,8-tetrahydrothiophene[2,3- b ][1,6]Naphthyridine-2-carboxamide as a novel multifunctional acetylcholinesterase inhibitor. Background technique [0002] Alzheimer's disease (AD) is a progressive, multifactorial, fatal neurodegenerative disease. The clinical manifestations are cognitive impairment and abnormal behavior of patients. According to the World Alzheimer's Disease Report, the number of AD patients in the world was 46 million in 2015, and it is expected that the number of patients will reach 130 million by 2050. [0003] The etiology and pathogenesis of AD are extremely unclear, while choline dysfunction, amyloid-β (Aβ) aggregation, and tau protein phosphorylation are considered to play important roles in the development of AD. However, the clinical trials of drugs targeting Aβ and tau pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/14A61K31/4375A61P25/28
Inventor 张娟江成世张华朱孔凯成志强宋佳丽葛永喜
Owner UNIV OF JINAN
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