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Benzothiazole derivative and application thereof

A technology of benzothiazole derivatives, which is applied in the field of benzothiazole derivatives, can solve the problems of slow brain clearance, postmortem diagnosis, large trauma and risk of biopsy

Inactive Publication Date: 2012-07-11
HEFEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current detection methods mainly include biopsy and histological analysis of autopsy, etc. Both methods have obvious defects: biopsy has greater trauma and risk, and autopsy can only be used for postmortem diagnosis, etc.
in,[ 125 I] TZDM, [ 125 I] Although IBOX can bind amyloid, it is cleared slowly in the brain of normal mice, indicating that there may be a high degree of non-specific binding in vivo

Method used

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  • Benzothiazole derivative and application thereof
  • Benzothiazole derivative and application thereof
  • Benzothiazole derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1: the synthetic method of benzothiazole Schiff base compound

[0052]

[0053] The synthesis of benzothiazole Schiff base compounds is formed by condensation of 2-aminobenzothiazole and substituted benzaldehyde, refluxed in ethanol, organic acid (such as acetic acid, p-toluenesulfonic acid) or Lewis acid (such as chlorine ZnC) catalysis.

Embodiment 2

[0054] Embodiment 2: the synthetic method of benzothiazole azo compound

[0055]

[0056] The synthesis of benzothiazole azo compounds firstly reacts 2-aminobenzothiazole and sodium nitrite at low temperature under acidic conditions to form diazonium salts, and then couples with aromatic compounds to obtain benzothiazole azo compounds.

Embodiment 3

[0057] Embodiment 3: benzothiazole derivatives 11 C radioisotope labeling method

[0058]

[0059] Benzothiazole derivatives 11 C radioisotope labeling includes the amino and hydroxyl groups on the aromatic ring 11 C radioactively labeled. Among them, the radioisotope modification of amino and methylamino can be obtained 11 C-labeled methylamino and dimethylamino; radioactive isotope modification of the phenolic hydroxyl group can be obtained 11 C labeled methoxy.

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Abstract

The invention discloses benzothiazole derivatives represented by general formulas (I)-(II) and pharmaceutically acceptable salts thereof, which have inhibition and developing effects on aggregation and precipitation of amyloid beta-protein. When being used as developers, the benzothiazole derivatives are required to be marked with appropriate radioactive isotopes or contrast agents which are applicable to magnetic resonance detection. The compounds are applied to producing drugs for preventing and treating diseases including Alzheimer's disease, and the developers are applied to aggregates and sediments of amyloid beta-protein.

Description

1. Technical field [0001] The present invention relates to a class of bioactive compounds and uses thereof, in particular to a benzothiazole derivative capable of imaging amyloid deposits and inhibiting their aggregation. 2. Background technology [0002] Alzheimer's disease (AD) is a common neurodegenerative disease, the main clinical manifestations are cognitive dysfunction and memory loss, personality and behavior changes, decreased judgment, loss of self-care ability, etc. human health and quality of life. Currently in developed countries, AD has become the fourth biggest killer after heart disease, tumor and stroke. Brain tissue autopsy confirmed to contain a large number of senile plaques (SPs) formed by the aggregation of β-amyloid protein (Aβ) and neurofibrillary tangles (NFTs) formed by hyperphosphorylated tau protein, as well as neuron loss, etc., among the present invention Reference to amyloid deposits includes, but is not limited to, senile plaques. [0003] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D277/82C07D417/12C07B59/00A61K31/4439A61K31/428A61K31/655A61K51/04A61P25/28A61P35/00A61P25/00
Inventor 甘昌胜周琳潘见
Owner HEFEI UNIV OF TECH
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