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目的设计并合成4-烷氧甲酰基苯并噁唑酮类化合物,并对其进行体外抗炎活性研究。方法以3-羟基-2-氨基苯甲酸为起始原料,经过酯化、成环和取代反应合成目标化合物,并对其进行结构确证。采用LPS诱导的小鼠巨噬细胞RAW264.7炎症模型,通过Griess法测定细胞培养液中NO的释放量,ELISA法测定细胞培养液中IL-6和IL-1β的量以评价化合物的体外抗炎活性。结果共合成了10个目标化合物,均通过ESI-MS、~1H-NMR及~(13)C-NMR对其结构进行确证。体外抗炎活性测定结果表明,化合物3d在25μmol/L时对IL-1β的抑制率达63.96%,对IL-6的抑制率达60.99%,与阳性对照药塞来昔布活性相当。结论 4-烷氧甲酰基苯并噁唑酮类化合物可通过抑制NO、IL-6和IL-1β炎症因子的释放而发挥抗炎活性。
Objective To design and synthesize 4-alkoxycarbonyl benzooxazolones and study their anti-inflammatory activity in vitro. Methods Starting from 3-hydroxy-2-aminobenzoic acid, the target compounds were synthesized through esterification, cyclization and substitution reactions. Their structures were confirmed. The LPS-induced mouse macrophage RAW264.7 inflammation model was used to determine the amount of NO released from the cell culture medium by Griess method. The amount of IL-6 and IL-1β in the cell culture medium was measured by ELISA to evaluate the in vitro anti- Inflammatory activity. Results A total of 10 target compounds were synthesized and their structures were confirmed by ESI-MS, ~ 1H-NMR and ~ (13) C-NMR. The results of in vitro anti-inflammatory activity assay showed that the inhibitory rate of compound 3d at 25μmol / L was 63.96% and that of IL-6 was 60.99%, which was comparable to the positive control drug celecoxib. Conclusion 4-Alkoxycarbonyl benzoxazolones exert anti-inflammatory activity by inhibiting the release of NO, IL-6 and IL-1β inflammatory cytokines.