A green synthetic approach to the synthesis of Schiff bases from 4-amino-2-thioxo-1,3-diazaspiro[5.5]undec-4-ene-5-carbonitrile as potential anti-inflammatory agents.

Bioorganicheskaia khimiia Pub Date : 2014-05-01
Sh A Abdel-Mohsen, E M Hussein
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Abstract

A green, novel, rapid, and efficient protocol is developed for the synthesis of various Schiffbases from 4-amino-2-thioxo-1,3-diazaspiro[5.5]undec-4-ene-5-carbonitrile using ammonium chloride as a very inexpensive and readily available reagent in refluxing ethanol. High yields, easy work-up, and short reaction times are advantages of this environmentally benign procedure. The prepared compounds were screened for their anti-inflammatory activity "at a dose of 10 mg/kg body weight", which revealed promising activities relative to indomethacin used as a reference standard in this study.

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以潜在抗炎剂4-氨基-2-硫氧基-1,3-重氮斯匹罗[5.5]十一-4-烯-5-碳腈为原料合成希夫碱的绿色合成方法
本文提出了一种绿色、新颖、快速、高效的方法,以4-氨基-2-硫氧基-1,3-重氮斯皮罗[5.5]十一-4-烯-5-碳腈为原料,利用氯化铵作为一种非常便宜和容易获得的试剂,在回流乙醇中合成各种希夫碱。产率高,易于处理,反应时间短是这种环境友好的程序的优点。制备的化合物在“10 mg/kg体重剂量下”的抗炎活性进行了筛选,相对于本研究使用的参考标准物吲哚美辛,具有较好的抗炎活性。
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