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Synthesis and Biological Evaluation of 3-Amino Pyrazolones

机译:3-氨基吡唑啉酮的合成及生物学评价

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摘要

A series of 3-amino-4-(substituted benzylidene)-1H-pyrazol-5(4H)-ones were synthesized by condensation of ethyl-2-cyano-3-(substi-tuted) phenylacrylates with hydrazine hydrate. The chemical structures of synthesized compounds were confirmed by means of IR, ~1H NMR, mass spectral and elemental analysis. All the compounds were screened for their antiinflammatory, analgesic and antioxidant activities. Out of these compounds, 4-hydroxy-3,5-dimethoxy (24) and 4-dimethylamino (17) derivatives showed good antiinflammatory activity. 4-dimethylamino (17) and 5-bromo-4-hydroxy-3-methoxy (23) derivatives showed moderate analgesic activity.
机译:通过将2-氰基-3-(取代的)苯基丙烯酸乙酯与水合肼缩合,合成了一系列3-氨基-4-(取代的亚苄基)-1H-吡唑-5(4H)-。通过IR,〜1H NMR,质谱和元素分析确认了合成化合物的化学结构。筛选所有化合物的抗炎,止痛和抗氧化活性。在这些化合物中,4-羟基-3,5-二甲氧基(24)和4-二甲基氨基(17)衍生物显示出良好的抗炎活性。 4-二甲基氨基(17)和5-溴-4-羟基-3-甲氧基(23)衍生物显示中等镇痛活性。

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