Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents

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• 作者：Juan Sun ; Su Wang ; Gui-Hua Sheng ; Zhi-Min Lian ; Han-Yu Liu ; Hai-Liang Zhu
• 关键词：Anti-inflammatory scaffold ; Cyclooxygenase-2 ; 1 ; 4-Benzodioxan ; Phenylpiperazine
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2016
• 出版时间：1 November 2016
• 年：2016
• 卷：24
• 期：21
• 页码：5626-5632
• 全文大小：1162 K

文摘

1-((2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-substituted-phenylpiperazine moiety was prepared and has been found to be a new and selective ligand for the enzyme cyclooxygenase-2 (COX-2). The biological activity of compound rong class="boldFont">3krong> as anti-inflammatory agent was further investigated both in vitro and in vivo. Notably, compound rong class="boldFont">3krong> exhibited the best anti-inflammatory activity among the eleven designed compounds with no toxicity, as determined by the ulcerogenic activity. Computational docking studies also showed that compound rong class="boldFont">3krong> has interaction with COX-2 key residues in the active site. Compound rong class="boldFont">3krong> maybe a new anti-inflammatory lead-candidate as powerful and novel non-ulcerogenic.