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Structure of drug for treating neurodegenerative disease

A drug and composition technology, applied in the field of new drug structure, can solve problems such as obvious adverse reactions

Inactive Publication Date: 2011-11-02
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, neurodegenerative diseases are still dominated by drug treatment. For example, the clinical drugs for the treatment of Parkinson's disease are mainly levodopa, which affects the dopaminergic nerve, and trihexyphenidyl, an anticholinergic drug. However, the adverse reactions of these drugs are obvious.

Method used

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  • Structure of drug for treating neurodegenerative disease
  • Structure of drug for treating neurodegenerative disease
  • Structure of drug for treating neurodegenerative disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: the synthetic method of compound 1

[0020]

[0021] 1.22 g (10.0 mmol) of p-hydroxybenzaldehyde and 1.48 g (10.0 mmol) of dihydroxylamine were dissolved in 50 mL of methanol and refluxed for 24 h. A large amount of white insoluble matter was formed, filtered, and the filter cake was washed with a small amount of methanol. Suspend the filter cake in 50.0 mL CH 2 Cl 2 , cooled in an ice-water bath, and added 30.0 mL NaIO 4 (1.7 g) aqueous solution, the reaction was stopped after stirring for 15 min. After static separation, the aqueous phase was washed with CH 2 Cl 2 Extracted twice, combined the organic phases, dried overnight, filtered, removed the solvent under reduced pressure, and purified by column chromatography to obtain 1.12 g of the product, with a yield of 45%. Mp: 137-139℃.R f =0.33 (CHCl 3 / CH 3 OH, 20:1). EI-MS(m / z) 250.1[M] + .IR(KBr) 3340 (OH); 1590, 1450, 1380, 880, 800, 690 cm -1 . Anal. Calcd for C 13 h 17 N 2 o 3 : C,...

Embodiment 2

[0022] Embodiment 2: the synthetic method of compound 2

[0023]

[0024] 1.88 g (10.0 mmol) of p-2,4-dichlorobenzaldehyde and 1.48 g (10.0 mmol) of dihydroxylamine were dissolved in 50 mL of methanol and refluxed for 24 h. A large amount of white insoluble matter was formed, filtered, and the filter cake was washed with a small amount of methanol. Suspend the filter cake in 50.0 mL CH 2 Cl 2 , cooled in an ice-water bath, and added 30.0 mL NaIO 4 (1.7 g) aqueous solution, the reaction was stopped after stirring for 15 min. After static separation, the aqueous phase was washed with CH 2 Cl 2 Extract twice, combine the organic phases, dry overnight, filter, remove the solvent under reduced pressure, and purify by column chromatography to obtain 1.55 g of the product with a yield of 51%. Mp: 123-125℃.R f = 0.54(CHCl 3 / CH 3 OH, 20:1). EI-MS (m / z) 302 [M] + .IR (KBr) 1590, 1450, 1365, 1000, 825, 870 cm_1. Anal. Calcd for C 13 h 15 N 2 o 2 Cl 2 : C, 51.67; H, ...

Embodiment 3

[0025] Embodiment 3: the synthetic method of compound 3

[0026]

[0027] 1.53 g (10.0 mmol) of p-fluoroformaldehyde and 1.48 g (10.0 mmol) of dihydroxylamine were dissolved in 50 mL of methanol and refluxed for 24 h. A large amount of white insoluble matter was formed, filtered, and the filter cake was washed with a small amount of methanol. Suspend the filter cake in 50.0 mL CH 2 Cl 2 , cooled in an ice-water bath, and added 30.0 mL NaIO 4 (1.7 g) aqueous solution, the reaction was stopped after stirring for 15 min. After static separation, the aqueous phase was washed with CH 2 Cl 2 Extract twice, combine the organic phases, dry overnight, filter, remove the solvent under reduced pressure, and purify by column chromatography to obtain 1.40 g of the product with a yield of 56%. Mp: 112-114℃. R f =0.52 (CHCl 3 / CH 3 OH, 20:1). EI-MS (m / z) 251 [M] + .IR (KBr) 1610, 1450, 1370, 1135, 770 cm -1 . Anal. Calcd for C 13 h 16 N 2 o 4 F: C, 55.11; H, 5.69; N, 9.88...

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Abstract

The invention discloses a drug structure as shown in the general formula (1), wherein, R1-R5 is independently selected from H, OH, halogen, NO2 or OR, R represents C1-C6 alkyl. The in vitro experiments of pharmacodynamics show that the compound can protect neurons, control Alzheimer disease, and the compound has obvious inhibiting effects to parkinsonism and other neurodegenerative diseases.

Description

technical field [0001] The invention provides a novel drug structure for protecting neurons and preventing and treating neurodegenerative diseases such as senile dementia and Parkinson's disease, and belongs to the technical field of medicine. Background technique [0002] Neurodegenerative diseases are a kind of chronic progressive nervous system degenerative diseases clinically manifested in different degrees of impairment of memory, sensory ability, judgment, thinking ability and motor ability. Such diseases mainly include Alzheimer's disease (that is, senile dementia), Parkinson's disease and spinal muscular atrophy. With the advent of the world's aging population, the incidence of neurodegenerative diseases is increasing year by year. At present, the elderly population over 60 years old in my country has exceeded 120 million, and neurodegenerative diseases have become serious diseases that threaten the health of the elderly. [0003] At present, neurodegenerative dise...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/22C07D233/30A61K31/4164A61P25/16A61P25/28
Inventor 王海波孙晓莉招明高石天尧
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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