Synthesis and in vivo Anti-inflammatory Evaluation of Piperazine Derivatives Containing 1,4-Benzodioxan Moiety

被引:8
作者
Liu, Zhi-Ping [1 ]
Gong, Chang-Da [2 ]
Xie, Long-Yan [2 ]
Du, Xiu-Li [2 ]
Li, Yang [2 ]
Qin, Jie [2 ]
机构
[1] Pingdingshan Univ, Sch Med, Pingdingshan 467000, Peoples R China
[2] Shandong Univ Technol, Sch Life Sci, Zibo 255049, Peoples R China
基金
中国国家自然科学基金;
关键词
Piperazine; 1,4-benzodioxan; crystal structure; anti-inflammatory activity; SELECTIVE COX-2 INHIBITORS; BIOLOGICAL EVALUATION; MOLECULAR DOCKING; DESIGN; ANALOGS;
D O I
10.17344/acsi.2018.4887
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Six piperazine derivatives 6a-f containing 1,4-benzodioxan moiety have been synthesized and characterized by H-1 NMR, ESI-MS and elemental analysis. The structure of 6d was further confirmed by single crystal X-ray diffraction. All these novel compounds were screened for their in vivo anti-inflammatory activity employing classical para-xylene-induced mice ear-swelling model. The results revealed that most of the target compounds showed significant anti-inflammatory activities, especially compound 6a with ortho-substituted methoxy group on the phenylpiperazine ring exhibited the best activity among the designed compounds.
引用
收藏
页码:421 / 426
页数:6
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