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含吡唑部分的4-氨基-1,2,4-三唑衍生物席夫碱的合成、抗氧化及镇痛活性

Synthesis, antioxidant and analgesic activities of Schiff bases of 4-amino-1,2,4-triazole derivatives containing a pyrazole moiety.

作者信息

Karrouchi K, Chemlal L, Taoufik J, Cherrah Y, Radi S, El Abbes Faouzi M, Ansar M

机构信息

Laboratory of Medicinal Chemistry, Faculty of Medicine and Pharmacy, University Mohammed V, Rabat, Morocco; LCAE, Department of Chemistry, Faculty of Sciences, University Mohamed I, Oujda, Morocco.

Laboratory of Pharmacology and Toxicology, Pharmacokinetic Research Team, Faculty of Medicine and Pharmacy, University Mohammed V, Rabat, Morocco.

出版信息

Ann Pharm Fr. 2016 Nov;74(6):431-438. doi: 10.1016/j.pharma.2016.03.005. Epub 2016 Apr 20.

Abstract

A series of Schiff bases of 4-amino-1,2,4-triazole derivatives containing pyrazole (5a-h) were synthesized from condensation of 4-amino-5-(5-methyl-1H-pyrazol-3-yl)-4H-1,2,4-triazole-3-thiol (3) derivative with various aromatic aldehydes (4a-h). The structures of the synthesized compounds were elucidated by IR, H NMR, C NMR, and mass spectrometry. All the synthesized compounds (5a-h) were screened for their in vivo analgesic and in vitro antioxidant activities revealing significant analgesic and antioxidant properties.

摘要

通过4-氨基-5-(5-甲基-1H-吡唑-3-基)-4H-1,2,4-三唑-3-硫醇(3)衍生物与各种芳香醛(4a-h)缩合,合成了一系列含吡唑的4-氨基-1,2,4-三唑衍生物席夫碱(5a-h)。通过红外光谱、氢核磁共振、碳核磁共振和质谱对合成化合物的结构进行了阐明。对所有合成化合物(5a-h)进行了体内镇痛和体外抗氧化活性筛选,结果显示它们具有显著的镇痛和抗氧化特性。

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