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Phenylidene phenyl peptide compounds and medicinal composition and application thereof

A technology of benzylidene phenylene peptides and compounds, applied in the preparation of monoamine oxidase B inhibitors, the application field in medicine, to achieve the effect of novel structure and easy synthesis

Active Publication Date: 2018-11-06
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The compound of formula (I) of the present invention has the potential to become a selective MAO-B inhibitor, and so far there has been no relevant report on the compound in the treatment of PD

Method used

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  • Phenylidene phenyl peptide compounds and medicinal composition and application thereof
  • Phenylidene phenyl peptide compounds and medicinal composition and application thereof
  • Phenylidene phenyl peptide compounds and medicinal composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Compounds of the present invention are partly purchased from Holland specs company (website: http: / / www.specs.com), the corresponding numbers of the compounds in this part of the library are as follows:

[0048] compound

Embodiment 2

[0050]

Embodiment 3

[0053] Compound 32

[0054] (Z)-3-(4-methoxybenzylidene)isobenzofuran-1(3H)-one

[0055]

[0056] 1 H NMR (400MHz, CDCl 3 )δ7.93(d, J=7.6Hz, 1H), 7.82(d, J=8.8Hz, 2H), 7.72(m, 2H), 7.52(t, J=7.2Hz, 1H), 6.95(d, J=8.8Hz,2H),6.39(s,1H),3.86(s,3H).

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PUM

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Abstract

The invention provides phenylidene phenyl peptide compounds, a medicinal composition using the phenylidene phenyl peptide compounds as active components, and application thereof as monoamine oxidase B(MAO-B) inhibitors and application thereof to preparation of medicines for treating Parkinson's disease (PD). Monoamine oxidase B (MAO-B) has been proved to be closely related to the pathogenesis ofthe Parkinson's disease (PD) and is a classic target for research and development of the medicines for treating the Parkinson's disease (PD). The invention provides application of the phenylidene phenyl peptide compounds to preparation of the monoamine oxidase B (MAO-B) inhibitors. In-vitro kinase activity experiments prove that the phenylidene phenyl peptide compounds have a significant monoamineoxidase B (MAO-B) inhibiting effect.

Description

technical field [0001] The present invention relates to the field of medical technology, in particular to benzylidene phenylene peptide compounds, pharmaceutical compositions using them as active ingredients, and their application in the preparation of monoamine oxidase B (Monoamine Oxidase B, MAO-B) inhibitors, and their Application in preparation of medicine for treating Parkinson's Disease (PD). Background technique [0002] Parkinson's disease (PD) is a common neurodegenerative disease with an average age of onset of about 60 years old, which seriously endangers the health of the elderly and has a huge impact on society and economy. The main pathological change of Parkinson's disease is the degeneration and death of dopamine (DA) neurons in the substantia nigra of the basal ganglia, which leads to a significant decrease in the content of DA in the striatum and causes the disease. [0003] Monoamine Oxidase (MAO) is an enzyme that catalyzes the oxidative deamination reac...

Claims

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Application Information

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IPC IPC(8): C07D307/88C07D405/06C07D307/92A61P25/16A61K31/365A61K31/443
CPCC07D307/88C07D307/92C07D405/06
Inventor 左之利孙威彭佳乐孔德信周业珩
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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