Design, synthesis and biological evaluation of piperic acid triazolyl derivatives as potent anti-inflammatory agents

被引：19

作者：

Ali, Yakub ^{[1
]}

Alam, Mohammad Sarwar ^{[1
]}

Hamid, Hinna ^{[1
]}

Husain, Asif ^{[2
]}

Bano, Sameena ^{[1
]}

Dhulap, Abhijeet ^{[3
]}

Kharbanda, Chetna ^{[1
]}

Nazreen, Syed ^{[1
]}

Haider, Saqlain ^{[1
]}

机构：

[1] Jamia Hamdard, Fac Sci, Dept Chem, New Delhi 110062, India

[2] Jamia Hamdard, Fac Pharm, Dept Pharmaceut Chem, New Delhi 110062, India

[3] CSIR, Unit Res & Dev Informat Prod, Pune 411038, Maharashtra, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2015年 / 92卷

关键词：

Piperine; Click chemistry; TNF-alpha; Cytotoxicity; Immunohistochemistry; Molecular docking; ASSAY; ALPHA;

D O I：

10.1016/j.ejmech.2015.01.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Nineteen novel piperine based triazoles have been synthesized using click chemistry approach and were tested for in vivo anti-inflammatory activity. The most active compounds were evaluated for in vitro TNF-alpha expression. Compounds 3g and 3f were found to show significant in vivo inhibition of inflammation, 80.40% and 76.71%, respectively after 5 h in comparison to piperine (54.72%) and the standard drug indomethacin (77.02%) without causing any damage to the stomach. Compounds 3g and 3f suppressed TNF-a level by 73.73% and 70.64%, respectively and protein expression of COX-2, NF-kappa B and TNF-alpha more than indomethacin. Moreover, the compound 3g was found to show significant analgesic activity of 54.09% which was comparable with the indomethacin (57.43%). (C) 2015 Elsevier Masson SAS. All rights reserved.

引用

页码：490 / 500

页数：11

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