一些含苯丙氨酸部分的新型1,3,4-噻二唑和1,2,4-三唑化合物的合成及生物活性
Synthesis and biological activity of some new 1,3,4-thiadiazole and 1,2,4-triazole compounds containing a phenylalanine moiety.
作者信息
Moise Mihaela, Sunel Valeriu, Profire Lenuta, Popa Marcel, Desbrieres Jacques, Peptu Cristian
机构信息
Department of Organic Chemistry and Biochemistry, Faculty of Chemistry, Al. I. Cuza University, Iasi, 11 B-dul Carol I, 700506, Romania.
出版信息
Molecules. 2009 Jul 16;14(7):2621-31. doi: 10.3390/molecules14072621.
New 1,3,4-thiadiazole, 6, 7 and 1,2,4-triazole derivatives, 8, 9 containing a phenylalanine moiety have been synthesized by intramolecular cyclization of 1,4-disubstituted thiosemicarbazides, 4, 5, in acid and alkaline media, respectively; the thiosemicarbazides were obtained by reaction of hydrazide 3 with appropriate aromatic isothiocyanates. The toxicity of the synthesized compounds was evaluated and the anti-inflammatory study of the triazole compound 9 established an appreciable anti-inflammatory activity that is comparable with that of other nonsteroidal anti-inflammatory agents.
分别通过在酸性和碱性介质中使1,4 - 二取代硫代氨基脲（4,5）进行分子内环化反应，合成了含苯丙氨酸部分的新型1,3,4 - 噻二唑衍生物（6,7）和1,2,4 - 三唑衍生物（8,9）；硫代氨基脲是通过酰肼（3）与适当的芳香异硫氰酸酯反应制得的。对合成化合物的毒性进行了评估，并且对三唑化合物（9）的抗炎研究表明其具有明显的抗炎活性，可与其他非甾体抗炎药相媲美。
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