几种新型查尔酮类抗炎药的合成及生物学评价。

Q3 Pharmacology, Toxicology and Pharmaceutics

Current drug discovery technologies Pub Date : 2023-01-01 DOI:10.2174/1570163819666220613153225

Zia Ur Rehman, Pooja Saini, Sushil Kumar

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引用次数: 2

摘要

目的:制备一系列1-(4-(2-(1h -吲哚-1-基)-2-氧乙氧基)苯基)-3-苯基丙烷-2-烯-1- 1衍生物。方法:吲哚与氯乙酰氯在苯中反应得到主要化合物，得到2-氯-1-(吲哚-1-基)乙酮，在乙腈存在下与羟基苯乙酮反应生成2-(4-乙酰基苯氧基)-1-(1h -吲哚-1-基)乙二酮，然后经醛醇缩合得到各种最终衍生物。结果与结论:化合物合成后，通过溶解度、熔点、薄层色谱、IR、1HNMR光谱数据和元素分析等方法对合成的化合物进行了表征。采用角叉菜胶致大鼠后肢水肿模型，评价所制衍生物对wistar白化大鼠的抗炎活性。

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Synthesis and Biological Evaluation of Some New Chalcone Derivatives as Anti-inflammatory Agents.

Aim: The present research work aims to prepare a series of 1-(4-(2-(1H-indol-1-yl)-2- oxoethoxy)phenyl)-3-phenylprop-2-en-1-one derivatives.

Methods: The major compound was achieved by the reaction of indole with chloroacetylchloride in benzene afforded 2-chloro-1-(indoline-1-yl) ethanone which reacts o- hydroxy acetophenone in presence of acetonitrile to form 2-(4-acetylphenoxy)-1-(1H-indol-1-yl)ethan-1-one then goes through aldol condensation to give various final derivatives.

Results and conclusion: After the synthesis of compounds, the synthesized compounds were characterized by checking their solubility, melting point, thin layer chromatography, IR, 1HNMR spectral data and elemental analysis. All of the prepared derivatives were evaluated for their anti-inflammatory activity on wistar albino rats by following the carrageenan-induced Rat Hind Paw Edema model.

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来源期刊

Current drug discovery technologies Pharmacology, Toxicology and Pharmaceutics-Drug Discovery

CiteScore

3.70

自引率

0.00%

发文量

期刊介绍： Due to the plethora of new approaches being used in modern drug discovery by the pharmaceutical industry, Current Drug Discovery Technologies has been established to provide comprehensive overviews of all the major modern techniques and technologies used in drug design and discovery. The journal is the forum for publishing both original research papers and reviews describing novel approaches and cutting edge technologies used in all stages of drug discovery. The journal addresses the multidimensional challenges of drug discovery science including integration issues of the drug discovery process.