Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 3, Pages 602-606Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.12.008
Keywords
Inflammation; Chalcone; Derivatives; Anti-inflammatory activity; COX-2
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Funding
- Natural Science Foundation of Zhejiang Province of China [LY12H30001]
- high level innovation team and outstanding scholar project of Guangxi institutions of higher education [[2014] 49]
- Postdoctoral Science Foundation of Guangxi Province of China [Y201001928]
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In this study, two series of 35 new chalcone derivatives containing aryl-piperazine or aryl-sulfonyl-piperazine fragment were synthesized and their structures were characterized by H-1, C-13 and ESI-MS. The in vivo and in vitro anti-inflammatory activities of target compounds were evaluated by using classical para-xylene-induced mice ear-swelling model and ELISA assays. Furthermore, docking studies were performed in COX-2 (4PH9). The in vivo anti-inflammatory assays indicated that most of the target compounds showed significant anti-inflammatory activities. Docking results revealed that the anti-inflammatory activities of compounds correlated with their docking results. Especially, compound 6o exhibited the most potent anti-inflammatory activity in vivo with the lowest docking score of -17.4 kcal/mol and could significantly inhibit the release of LPS-induced IL-6 and TNF-alpha in a dose-dependent manner in vitro. (C) 2016 Elsevier Ltd. All rights reserved.
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