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Synthesis,Anti-inflammatory,Analgesic and Antipyretic Activity of Novel 1,3,5-Trisubstituted Pyrazole Derivatives

机译:新型1,3,5-三取代的吡唑衍生物的合成,抗炎,镇痛和解热活性

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A novel series of 1,3,5-trisubstituted pyrazole derivatives were synthesized by the cycloaddition reaction between the electron rich N-substituted aryl hydrazones and nitro-olefins.Different N-substituted aryl hydrazones(la-j)on reacting with 4-methyl-β-nitrostyrene(2)in ethylene glycol or trifluoroethanol-trifluoro acetic acid mixture(for acid stable hydrazones)at 120 °C,yielded various 1,3,5-trisubstituted pyrazoles(3a-j).The final products were characterized by spectral analysis using Mass,NMR and IR spectroscopy.All the products were assessed for their anti-inflammatory,analgesic and antipyretic activities on Swiss albino rats.All the compounds(3a-j)exhibited noteworthy defence against inflammation,nociception and hyperthermia.Compounds(3e and 3h)disclosed better antiinflammatory,analgesic and antipyretic activities while compound 3c had highest anti-inflammatory activity compared to the standard nimesulide.
机译:通过电子富氮的N-取代的芳基腙和硝基 - 烯烃之间的环加成反应合成了一种新的1,3,5-三取代的吡唑衍生物。用4-甲基反应的二十异子N-取代的芳基腙(LA-J)进行了二次取代的芳基腙(La-J) - 乙二醇或三氟乙醇 - 三氟乙酸混合物(用于酸稳定腙)的-β-硝基丁烯(2),得到各种1,3,5-三取代的吡嗪(3a-j)。最终产品 使用质量,NMR和IR光谱分谱的光谱分析。将产品评估其对瑞士白化大鼠的抗炎,镇痛和解热活性。所有化合物(3A-J)表现出对抗炎症,Nocieption和Hymerthima.comPounds的不值守防御( 图3E和3H)公开了更好的抗炎,镇痛和解热活性,而化合物3C与标准的尼菊酯相比具有最高的抗炎活性。

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