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题名: Discovery of potential anti-inflammatory drugs: diaryl-1,2,4-triazoles bearing N-hydroxyurea moiety as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase
作者: Jiang, Bo1,2,3; Huang, Xiaojing1,2; Yao, Hequan1,2; Jiang, Jieyun4; Wu, Xiaoming1,2; Jiang, Siyi5; Wang, Qiujuan5; Lu, Tao6; Xu, Jinyi1,2
刊名: ORGANIC & BIOMOLECULAR CHEMISTRY
出版日期: 2014
卷号: 12, 期号:13, 页码:2114-2127
学科分类: Chemistry
DOI: 10.1039/c3ob41936c
通讯作者: Wu, XM (reprint author), China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China.
文章类型: Article
英文摘要: A series of hybrids from diaryl-1,2,4-triazole and hydroxamic acid or N-hydroxyurea were synthesized and evaluated as novel anti-inflammatory agents. The biological data showed that (i) all the compounds showed dual COX-2/5-LOX inhibitory activities in vitro, and 15e showed optimal inhibitory activities (COX-2: IC50 = 0.15 mu M, 5-LOX: IC50 = 0.85 mu M), (ii) 15e selectively inhibited COX-2 relative to COX-1 with selectivity index (SI = 0.012) comparable to celecoxib (SI = 0.015), (iii) 15e exhibited potent anti-inflammatory activity (inhibition: 54.1%) which was comparable to the reference drug celecoxib (inhibition: 46.7%) in a xylene-induced ear edema assay, and (iv) 15e displayed promising analgesic activity in acetic acid-induced writhing response and hot-plate assay. Finally, a molecular modeling study revealed the binding interactions of 15e with COX-2 and 5-LOX. Our findings suggest that 15e may be a promising anti-inflammatory agent for further evaluation.
收录类别: SCI ; IC
语种: 英语
WOS记录号: WOS:000332457800015
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.qdio.ac.cn/handle/337002/24205
Appears in Collections:海洋生物技术研发中心_期刊论文

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作者单位: 1.China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
2.China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China
3.Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China
4.Univ Kentucky, Coll Med, Dept Microbiol Mol Genet & Immunol, Lexington, KY 40536 USA
5.China Pharmaceut Univ, Dept Physiol, Nanjing 210009, Jiangsu, Peoples R China
6.China Pharmaceut Univ, Lab Mol Design & Drug Discovery, Nanjing 211198, Jiangsu, Peoples R China
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文件名: Discovery of potential anti-inflammatory drugs diaryl-1,2,4-triazoles bearing N-hydroxyurea moiety as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.pdf
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