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Application of dicarboxylic acid and ester compounds thereof

A compound and drug technology, applied in the application field of preparing neuroprotective drugs, can solve problems such as side effects, inability to apply clinically, and poor effects

Inactive Publication Date: 2014-04-09
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, many protective reagents developed for different links of the cerebral infarction cascade reaction, except for the free radical scavenger Edaravone, are all effective in animals, clinically ineffective or poorly effective, or cannot be used in clinical practice due to serious side effects

Method used

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  • Application of dicarboxylic acid and ester compounds thereof
  • Application of dicarboxylic acid and ester compounds thereof
  • Application of dicarboxylic acid and ester compounds thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 The protective effect of compounds on glutamate-induced primary neuron cell damage

[0027] Experimental principle:

[0028] In this experiment, lactate dehydrogenase (Lactate dehydrogenase, LDH) assay was used. LDH exists in the cell, and the extracellular content is less under normal circumstances. When the cell is damaged, LDH will be released to the outside of the cell. Therefore, the degree of cell damage can be determined by detecting the leakage rate of LDH. LDH can catalyze lactic acid to generate pyruvic acid, and pyruvic acid reacts with 2,4-dinitrophenylhydrazine to generate pyruvic acid dinitrophenylhydrazone, which is brownish red in alkaline solution, and the enzyme activity can be determined by colorimetry.

[0029] Extraction of primary neurons from mouse cortex:

[0030] ICR pregnant mice with a gestational age of 15-16 days were taken. After the cervical vertebrae were dislocated, the uterus and placenta were separated, and the taken out fe...

Embodiment 2

[0056] Example 2 Neuroprotective effect of N-(2-methoxycarbonylacetyl)-D-valine methyl ester (ZLc-002) (1) on animal models

[0057] Preparation of N-(2-methoxycarbonylacetyl)-D-valine methyl ester (ZLc-002):

[0058] Add 1.50g (9mmol) of D-valine methyl ester hydrochloride to 35mL of dichloromethane at -15°C to dissolve, add 2.03mL (18.45mmol) of N-methylmorpholine dropwise, and stir for 5 minutes after dropping , and then added dropwise 1.02 mL (9.45 mmol) of monomethyl malonyl chloride, stirred for 30 minutes, and then continued to stir at 30° C. for 22 hours. Stop the reaction, evaporate the solvent to dryness, add 8 mL of water, 50 mL of ethyl acetate x 4 times of extraction, 25 mL of 10%wt citric acid x 2 times of washing, wash with saturated sodium chloride, and then 25 mL of 5%wt sodium bicarbonate x 2 times of washing, Then washed with saturated sodium chloride, dried over anhydrous sodium sulfate, filtered, the filtrate was evaporated to dryness, and the concentrate...

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Abstract

The invention provides an application of dicarboxylic acid and ester compounds thereof and in particular relates to an application of the compounds to preparation of neuroprotective drugs. In a chemical formula in the specification, R1 is hydrogen or methyl; R2 is isopropyl or isobutyl; R3 is carboxyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, borneol oxycarbonyl or 5-tetrazole; a is 0 or 1; b is 0 or 1; c is an integer from 1 to 4; b is 0 when a is 0; b is 0 or 1 when a is 1. The compounds have relatively strong protective effects on glutamate-induced neuron damages.

Description

technical field [0001] The invention belongs to the field of pharmacy, and provides the application of a class of dicarboxylic acid and its ester compound in the preparation of neuroprotective medicine. Background technique [0002] Neuroprotective agents are a hotspot in the development of therapeutic drugs for ischemic stroke. At present, many protective reagents developed for different links of the cerebral infarction cascade reaction, except for the free radical scavenger edaravone, are effective in animals, clinically ineffective or poorly effective, or cannot be used clinically due to serious side effects. Therefore, the development and screening of new neuroprotective agents is the focus of current research. [0003] Glutamate is released in large quantities when cerebral ischemia occurs. A large amount of glutamate released activates N-methylaspartic acid (NMDA) receptors, and calcium ions influx from NMDA receptors activate neuronal nitric oxide synthase (nNOS) an...

Claims

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Application Information

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IPC IPC(8): A61K31/225A61K31/22A61K31/20A61K31/198A61P25/00
Inventor 厉廷有丁屹蔡鋆鑫常磊李飞朱东亚
Owner NANJING MEDICAL UNIV
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