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

Zhi-Ping Liu, Chang-Da Gong, Long-Yan Xie, Xiu-Li Du, Yang Li, Jie Qin


Six piperazine derivatives 6af containing 1,4-benzodioxan moiety have been synthesized and characterized by 1H 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.


Piperazine; 1,4-benzodioxan; crystal structure; anti-inflammatory activity

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