首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, antioxidant activities and urease inhibition of some new 1,2,4-triazole and 1,3,4-thiadiazole derivatives.
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Synthesis, antioxidant activities and urease inhibition of some new 1,2,4-triazole and 1,3,4-thiadiazole derivatives.

机译:一些新的1,2,4-三唑和1,3,4-噻二唑衍生物的合成,抗氧化活性和脲酶抑制。

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摘要

New series of 4,5-disubstituted-2,4-dihydro-3H-1,2,4-triazole-3-thiones (8a-j) and 2,5-disubstituted-1,3,4-thiadiazoles (9a-h) were synthesized by dehydrative cyclization of hydrazinecarbothioamide derivatives (7a-k) by refluxing in 4N aqueous sodium hydroxide and by overnight stirring with polyphosphoric acid, respectively. The structures of the newly synthesized compounds were characterized by IR, (1)H NMR, (13)C NMR, elemental analysis and mass spectroscopic studies and the synthesized compounds were screened for their antioxidant and urease inhibition activities. N-(2,4-Dimethylphenyl)-5-(4-nitrophenyl)-1,3,4-thiadiazol-2-amine (9h) showed excellent antioxidant activity more than the standard drug whereas 4-(2,4-dimethylphenyl)-5-(3-nitrophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione (8d) and 4-(2,3-dimethylphenyl)-5-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione (8e) exhibited potent urease inhibitory activities.
机译:新的4,5-二取代-2,4-二氢-3H-1,2,4-三唑-3-酮(8A-J)和2,5-二取代-1,3,4-噻二唑(9A- 通过在4N氢氧化钠水溶液中回流并用多磷酸搅拌过夜,通过脱水环化通过脱水环化来合成肼基氨基噻嗪衍生物(7a-k)的脱水环化。 通过IR,(1)H NMR,(13)C NMR,元素分析和质谱研究,对新合成化合物的结构表征,并筛选合成化合物,用于其抗氧化剂和脲酶抑制活性。 N-(2,4-二甲基苯基)-5-(4-硝基苯基)-1,3,4-噻二唑-2-胺(9h)显示出优异的抗氧化活性,比标准药物多,而4-(2,4-二甲基苯基 )-5-(3-硝基苯基)-2,4-二氢-3H-1,2,4-三唑-3-倍硫基(8d)和4-(2,3-二甲基苯基)-5-苯基-2,4 -dihydro-3h-1,2,4-三唑-3-thione(8e)表现出有效的脲酶抑制活动。

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