首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and anti-inflammatory activity evaluation of some novel 6-alkoxy(phenoxy)-(1,2,4)triazolo(3,4-a)phthalazine-3-amine derivatives.
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Synthesis and anti-inflammatory activity evaluation of some novel 6-alkoxy(phenoxy)-(1,2,4)triazolo(3,4-a)phthalazine-3-amine derivatives.

机译:一些新型6-烷氧基(苯氧氧基) - (1,2,4)三唑(3,4-A)酞嗪-3-胺衍生物的合成与抗炎活性评价。

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摘要

Starting from phthalic anhydride, several new 6-alkoxy(phenoxy)-[1,2,4]triazolo[3,4-a]phthalazine-3-amine derivatives were synthesized as potent anti-inflammatory agent. The study showed that the compounds 6h (6-(2-chlorophenoxy)-[1,2,4]triazolo[3,4-a]phthalazine-3-amine) and 6s (6-(4-aminophenoxy)-[1,2,4] triazolo[3,4-a]phthalazine-3-amine) exhibited the highest anti-inflammatory activity (81% and 83% inhibition, respectively, at 0.5 h after i.p. administration) which were slightly more potent than the reference drug Ibuprofen (61%). Furthermore, the peak activity of 6h and 6s was observed at the 3 h after p.o. administration, and they exhibited stronger anti-inflammatory activity than Ibuprofen at the dose of 50 mg/kg at the peak time.
机译:从邻苯二甲酸酐开始,几种新的6-烷氧基(苯氧氧基) - [1,2,4]三唑唑[3,4-a]酞嗪-3-胺衍生物被合成为有效的抗炎剂。 该研究表明,化合物6H(6-(2-氯苯氧基) - [1,2,4]三唑泊[3,4-A]酞嗪-3-胺)和6s(6-(4-氨基苯甲酸) - [1 ,2,4]三唑唑[3,4-A]酞嗪-3-胺出现了最高的抗炎活性(分别为81%和83%抑制,在IP给药后0.5小时),其略高于 参考药物布洛芬(61%)。 此外,在P.O之后在3小时内观察到6小时和6s的峰值活性。 施用,它们在峰值时间以50mg / kg的剂量表现出比布洛芬更强的抗炎活性。

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