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Compound, composition and method for preventing from neurodegeneration in injury of central nervous system

A compound and composition technology, applied in the field of neurological diseases

Inactive Publication Date: 2007-04-04
GNT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the pathogenesis of ALS has not been elucidated, excitotoxicity is thought to be involved in the ALS process

Method used

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  • Compound, composition and method for preventing from neurodegeneration in injury of central nervous system
  • Compound, composition and method for preventing from neurodegeneration in injury of central nervous system
  • Compound, composition and method for preventing from neurodegeneration in injury of central nervous system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 5

[0057]

[0058] Reagent (a) N,N-methylformamide (DMF), triethylamine, room temperature, 4 hours.

[0059] Specific compounds of interest in formula (I) are as follows:

[0060] 5-Benzylaminosalicylic acid

[0061] 5-(4-nitrobenzyl)aminosalicylic acid (NBAS)

[0062] 5-(4-Chlorobenzyl)aminosalicylic acid (CBAS)

[0063] 5-(4-Trifluoromethylbenzyl)aminosalicylic acid (TBAS)

[0064] 5-(4-Fluorobenzyl)aminosalicylic acid (FBAS)

[0065] 5-(4-Methoxybenzyl)aminosalicylic acid (MBAS)

[0066] 5-(Pentafluorobenzyl)aminosalicylic acid (PBAS)

[0067] 5-(4-Nitrobenzyl)amino-2-hydroxybenzoic acid ethyl ester (NAHE)

[0068] 5-(4-Nitrobenzyl)-N-acetamido-2-hydroxybenzoic acid ethyl ester (NNAHE)

[0069] 5-(4-Nitrobenzyl)-N-acetamido-2-acetoxy-ethyl benzoate (NNAAE)

[0070] 5-(4-Nitrobenzoyl)aminosalicylic acid (NBAA)

[0071] 5-(4-Nitrobenzenesulfonyl)aminosalicylic acid (NBSAA)

[0072] 5-[2-(4-Nitrophenyl)-ethyl]aminosalicylic acid (NPAA)

[0073] 5-[3-(4-nitrophenyl)n...

experiment Embodiment 1

[0123] Experimental Example 1: Antioxidative Effect of 5-Aminosalicylic Acid

[0124] The neuroprotective effects of 5-aminosalicylic acid (AS) were tested in primary cortical cell cultures. Containing 10-300 μM AS did not reduce neuronal death induced by 10 min exposure to 300 μM NMDA over 24 hours (Fig. 1.a). Interestingly, adding 10-100 μM AS dose-dependently prevented free radical neurotoxicity induced by exposure to ferrous ions for 24 h (Fig. 1b). Continuous addition of AS during and after zinc ion treatment did not reduce neuronal death 24 hours after exposure to 300 micromolar zinc ions for 30 min. The neuroprotective effect of AS against free radical neurotoxicity is attributed to the direct antioxidant properties of the compound AS reducing the level of DPPH, a stable free radical. Compared to trolox, a membrane permeable form of vitamin E, AS is a weak oxidizing agent.

[0125] Reactant

Concentration of Trolox or AS (micromolar)

0

3...

experiment Embodiment 2

[0128] Experimental Example 2: Neuroprotective Effects of 5-Benzylaminosalicylic Acid and Its Derivatives

[0129] Neuroprotective effects of 1.5-benzylaminosalicylic acid

[0130] BAS was synthesized and tested for its ability to resist nerve damage induced in cortical cell cultures. Simultaneous addition of 300 micromolar 5-benzylaminosalicylic acid (BAS) was able to reduce NMDA-induced neuronal death by approximately 50% (Fig. 2a). In the presence of 1 μM BAS, there was a considerable decrease in neuronal death induced by exposure to 50 μM ferrous ions (Fig. 2b) or 10 mmol BSO (Fig. 2c), adding 3 μM molar BAs, neuronal death was essentially completely blocked. Addition of 30-300 micromolar BAS dose-dependently reduced neuronal death induced by exposure to 300 micromolar zinc ions for 30 minutes over 24 hours. Like AS or trolox, BAS is a direct antioxidant (Table 2). The antioxidant properties of BAS were observed at doses as low as 1 micromolar.

[0131] [BAS]...

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Abstract

A composition for preventing nervous diseases accompanied with neuron death, its method and synthesis of BAS and its derivative are disclosed. BAS and its derivative prevent cortical neuron from being damaged by N-methyl-D-aspartate, zinc ion and active oxide cluster. It can be used to treat apoplexia, cerebral traumatism, spinal injury, epilepsy and other neurodegenerative diseases, which accompany with serious neuron lost.

Description

technical field [0001] The present invention relates to novel salicylic acid compounds, compositions, and methods for preventing and preventing neurological diseases accompanied by neuronal death. Background technique [0002] Excitotoxicity and Brain Disease [0003] Hyperactivation of ionotropic glutamate receptors sensitive to N-methyl-D-aspartate (NMDA receptors) causes neuronal death and is known to mediate a variety of neurological disorders [Choi , Neuron 1:623-634 (1988)]. Glutamate is an excitatory neurotransmitter, which accumulates in large quantities in the brain and is susceptible to hypoxic-ischemic damage, which activates ionized glutamate receptors, making them accessible to calcium and sodium ions Infiltration, followed by neuronal death [Choi and Rothman, Annu Rev Neurosci: 13: 171-182 (1990)]. NMDA receptor antagonists significantly reduced hypoglycemia, hypoxia, and hypoxic-ischemia induced by brain injury [Simon, Swan, Griffiths, and Meldrum. Science...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/64C07C311/21A61K31/606A61P25/00A61P25/14A61P25/16A61P25/28C12M3/00A61BA61B17/42A61B17/435A61B19/02A61D19/02A61D19/04A61K31/196A61K31/618A61K31/621A61P3/10A61P7/06A61P19/08A61P21/04A61P25/08A61P43/00C07C233/54C07C233/81
CPCC07C233/54C07C229/64C07C311/21A61P19/08A61P21/04A61P25/00A61P25/08A61P25/14A61P25/16A61P25/28A61P43/00A61P7/06A61P9/10A61P3/10
Inventor 郭秉周李英爱柳宝凛尹性和文镐相
Owner GNT PHARMA
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