Synthesis and Biological Evaluation of Novel Phthalide Analogs-1,2,4-Oxadiazole Hybrids as Potential Anti-Inflammatory Agents
文献类型： 外文期刊
作者： Ruan, Banfeng 1 ; Tang, Xiaofei 1 ; Guo, Weiyun 1 ; Hu, Yong 2 ; Chen, Liuzeng 1 ;
作者机构： 1.Hefei Univ, Key Lab Biofabricat Anhui Higher Educ, Hefei 230601, Peoples R China
2.Anhui Acad Agr Sci, Agroprod Proc Res Inst, Hefei 230001, Peoples R China
关键词： phthalide derivatives; 1; 2; 4-oxadiazole; hybrids; anti-inflammatory activity; SAR
期刊名称：CHEMISTRY & BIODIVERSITY （ 影响因子：2.745； 五年影响因子：2.581 ）
ISSN： 1612-1872
年卷期：
页码：
收录情况： SCI
摘要： A series of novel pathalide-1,2,4-oxadiazole analogs were synthesized for discovering novel anti-inflammatory agents. After the assessment of their cytotoxicity in vitro, all compounds had been screened for their anti-inflammatory activity by evaluating their inhibitory effect on LPS-induced NO production in RAW 264.7 macrophages. SARs had been concluded, and finally compound E13 was found to be the most potent compound. This compound could also significantly decrease the production of iNOS and COX-2. Preliminary mechanism studies indicated that compound E13 could inhibit the TLR4/NF-kappa B and ERK/p38 signaling pathways. These findings indicate that E13 holds great potential to be a lead compound for discovering novel anti-inflammatory drugs.
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