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A kind of benzylamino acid derivatives and its application in the preparation of anti-inflammatory drugs

An anti-inflammatory drug and pharmacy technology, applied in the field of benzylaminoyl derivatives, the preparation of anti-inflammatory drugs, and can solve the problems of increased nitrite/nitrate levels and the like

Active Publication Date: 2022-03-29
CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, administration of the compounds disclosed therein may be accompanied by increases in blood nitrite / nitrate levels which are considered unfavorable

Method used

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  • A kind of benzylamino acid derivatives and its application in the preparation of anti-inflammatory drugs
  • A kind of benzylamino acid derivatives and its application in the preparation of anti-inflammatory drugs
  • A kind of benzylamino acid derivatives and its application in the preparation of anti-inflammatory drugs

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Experimental program
Comparison scheme
Effect test

experiment example 1

[0056] Synthesis of experimental example 1 compound of the present invention

[0057] Compound 2:

[0058]

[0059]N-(3,4-dimethoxybenzyl)nonanamide (0.154g, 0.5mmol) was dissolved in anhydrous dichloromethane (10mL), added boron tribromide (57μL, 0.6mmol)-reacted at room temperature for 2h, added water 30mL, ethyl acetate 50mL, 0.5g citric acid, stirred for 2h, the ethyl acetate solution was dehydrated with anhydrous sodium sulfate, ethyl acetate was recovered, and the residue was subjected to silica gel column chromatography (petroleum ether-ethyl acetate (3:1)) to obtain the compound 2 (0.112 g, 80%). 1H NMR (400MHz, CDCl 3 )δ8.44(s,1H),6.86(d,J=1.9Hz,1H),6.83(d,J=8.0Hz,1H),6.64(dd,J=8.0,2.0Hz,1H),6.26( s,1H,OH),6.01(s,1H,OH),4.32(d,J=5.9Hz,2H),2.32–2.17(m,2H),1.70–1.55(m,2H),1.27(q, J=7.5,6.7Hz,10H),0.89(t,J=6.9Hz,3H); 13 C NMR (101MHz, DMSO-D 6 ) δ 172.4, 145.5, 144.5, 131.0, 118.6, 115.7, 115.4, 42.1, 35.9, 31.7, 29.2, 29.2, 29.1, 25.8, 22.6, 14.4.

[0060] Com...

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PUM

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Abstract

The present invention provides the compound represented by formula A, or its pharmaceutically acceptable salt, or its solvate, and its use in the preparation of anti-inflammatory drugs. Experiments have proved that the compound represented by formula A prepared by the present invention can significantly inhibit LPS-induced NO production, has strong anti-inflammatory ability, and has low cytotoxicity, and can be applied to the preparation of clinical anti-inflammatory drugs.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to a benzylamide derivative and its use in the preparation of anti-inflammatory drugs. Background technique [0002] As an important pathological process, inflammation is very common in the human body, and it itself is an autoimmune response of the body to external or foreign body stimuli. And when this response is dysregulated or excessively responds to the body's self-injury, it evolves into inflammation. Therefore, most diseases are accompanied by the mediation and occurrence of inflammation, and the mediation and occurrence of inflammation aggravate the damage to the body of the disease, such as acute lung injury, rheumatoid arthritis, diabetes complications, cancer, atherosclerosis sclerosis, inflammatory bowel disease, etc. In these processes, proinflammatory factors such as TNF-α, IL-6, IL-1β, etc. have played an important role. [0003] At present, there are m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C233/18C07C233/29C07C231/12A61P29/00A61K31/165A61K31/221
Inventor 张国林王飞卢晓霞闻永举周宗元
Owner CHENGDU INST OF BIOLOGY CHINESE ACAD OF S