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Molecules 2016, 21(11), 1544;

Synthesis, Characterization, and Anti-Inflammatory Activities of Methyl Salicylate Derivatives Bearing Piperazine Moiety

Department of Life Science, Huzhou Teachers’ College, Huzhou 313000, China
School of Chemistry and Chemical Engineering, Guangxi University, Nanning 530004, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 11 October 2016 / Revised: 10 November 2016 / Accepted: 11 November 2016 / Published: 23 November 2016
(This article belongs to the Section Medicinal Chemistry)
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In this study, a new series of 16 methyl salicylate derivatives bearing a piperazine moiety were synthesized and characterized. The in vivo anti-inflammatory activities of target compounds were investigated against xylol-induced ear edema and carrageenan-induced paw edema in mice. The results showed that all synthesized compounds exhibited potent anti-inflammatory activities. Especially, the anti-inflammatory activities of compounds M15 and M16 were higher than that of aspirin and even equal to that of indomethacin at the same dose. In addition, the in vitro cytotoxicity activities and anti-inflammatory activities of four target compounds were performed in RAW264.7 macrophages, and compound M16 was found to significantly inhibit the release of lipopolysaccharide (LPS)-induced interleukin (IL)-6 and tumor necrosis factor (TNF)-α in a dose-dependent manner. In addition, compound M16 was found to attenuate LPS induced cyclooxygenase (COX)-2 up-regulation. The current preliminary study may provide information for the development of new and safe anti-inflammatory agents. View Full-Text
Keywords: inflammation; salicylate; piperazine; derivatives; anti-inflammatory activity inflammation; salicylate; piperazine; derivatives; anti-inflammatory activity

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Li, J.; Yin, Y.; Wang, L.; Liang, P.; Li, M.; Liu, X.; Wu, L.; Yang, H. Synthesis, Characterization, and Anti-Inflammatory Activities of Methyl Salicylate Derivatives Bearing Piperazine Moiety. Molecules 2016, 21, 1544.

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