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Synthetic method of acetaldehyde dehydrogenase activator alda-1, and application of same

A technology of acetaldehyde dehydrogenase and activator, which is applied in the field of biomedicine, can solve the problems that the new compound alda-1 has few reports, no research, and cannot effectively enter the brain and central nervous system, so as to simplify the synthesis route, The effect of expanding indications and enhancing compliance

Inactive Publication Date: 2013-07-10
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, animal experiments on the cardioprotective effect of adla-1 have been reported, but almost all macromolecular and 95% small molecule drugs are difficult to pass through the blood-brain barrier and cannot effectively enter the brain and central nervous system. Can adla-1 be used? The research on protecting cerebrovascular injury has not been reported in the literature
In addition, there are very few reports on the new compound alda-1. The main research is that the antioxidant effect of alda-1 is related to myocardial protection. Whether the oral preparation can reach the brain through the blood-brain barrier has not yet been studied.

Method used

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  • Synthetic method of acetaldehyde dehydrogenase activator alda-1, and application of same
  • Synthetic method of acetaldehyde dehydrogenase activator alda-1, and application of same
  • Synthetic method of acetaldehyde dehydrogenase activator alda-1, and application of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Synthesis of alda-1

[0026] Add 8.50g (56.2mmol) of piperonylamine into a 500ml round bottom flask equipped with magnetic stirring, add 100ml of N,N'-dimethylformamide (DMF), cool and stir in an ice-water bath for 10 minutes, add 2,6- Dichlorobenzoic acid 11.77g (61.6mmol), dicyclohexylcarbodiimide (DCC) 12.95g (62.8mmol), 1-hydroxybenzotriazole (HOBT) 1.52g (11.3mmol), continue stirring for 30 minutes, remove Ice-water bath, stirring at room temperature for 12 hours. Thin-layer chromatography detects that the conversion of 2,6-dichlorobenzoic acid is complete, cooling and stirring in an ice-water bath for 1 hour, filtering, and washing the filter cake with 20ml of ice-cold DMF, combining the filtrate and washings, and transferring to a 1000ml three-necked round-bottomed flask with mechanical stirring 600ml of deionized water was added dropwise within 2 hours. After the dropwise addition was completed, the stirring was continued for 1 hour, filtered, and th...

Embodiment 2ald

[0028] Embodiment 2 preparation of alda-1 compressed tablet

[0029] Table 1 prepares the used raw materials of alda-1 compressed tablet and the dosage used for pressing 1000 tablets

[0030]

[0031]

[0032] Preparation process: mix alda-1, microcrystalline cellulose, crospovidone and magnesium stearate evenly, and then compress into tablets.

Embodiment 3

[0033] Embodiment 3: animal experiments

[0034] The distribution of whole body tissues at different time after gavage of alda-1 in rats

[0035] Table 2 Changes of drug content in various tissues at different times after gavage of alda-1 to rats

[0036] (ng equivalent / g or mL, mean ± SD, n=5)

[0037]

[0038] The distribution of total radioactivity at different times after gavage of alda-1 to rats is shown in Table 2. The distribution of total radioactivity in plasma and several important tissues at different times after intragastric administration of alda-1 was as follows: plasma, kidney, heart, liver, and brain. Less spleen, muscle, fat and bone marrow.

[0039] Protective effect of Alda-1 on cerebral ischemia-reperfusion injury

[0040] Implemented drugs: carboxymethylcellulose sodium (CMC-Na) was purchased from Shanghai Shanpu Chemical Co., Ltd.

[0041] The alda-1 compound prepared in Example 1 was prepared into a suspension using 0.5% carboxymethylcellulose so...

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Abstract

The invention relates to the field of biological medicines, in particular relates to a preparation method of acetaldehyde dehydrogenase activator alda-1, and application of the same. The acetaldehyde dehydrogenase activator alda-1 provided by the invention can be used for treating brain tissue nervous disease, in particular, has protection effect on cerebral ischemia-reperfusion. The acetaldehyde dehydrogenase activator alda-1 provided by the invention can be mixed with pharmaceutic adjuvant according to certain proportion so as to be prepared into any oral taken preparation, and the dosage of per unit of preparation is 5-500mg.

Description

technical field [0001] The present invention belongs to the field of biomedicine; the present invention provides a synthesis process of acetaldehyde dehydrogenase activator alda-1; the present invention also provides new uses and administration methods of the compound, including the protection against cerebral ischemia-reperfusion role, expanding the scope of alda-1 indications. Through the pharmacokinetic characteristics, the route of administration of the compound is improved. Background technique [0002] Cerebrovascular disease is a common and frequently-occurring disease that seriously endangers human health. It has become the first cause of disability and the third cause of death in the world. The incidence of ischemic cerebrovascular disease accounts for about 75% of cerebrovascular diseases. Currently recognized as an effective method is thrombolytic therapy, but limited by the time window and treatment conditions of thrombolytic therapy, only about 3% of patients c...

Claims

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Application Information

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IPC IPC(8): A61K31/36A61P9/10A61P9/00C07D317/58
Inventor 彭军付四海张洪峰
Owner CENT SOUTH UNIV
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