目的 設(shè)計(jì)并合成4-烷氧甲酰基苯并（口惡）唑酮類化合物，并對(duì)其進(jìn)行體外抗炎活性研究。方法 以3-羥基-2-氨基苯甲酸為起始原料，經(jīng)過酯化、成環(huán)和取代反應(yīng)合成目標(biāo)化合物，并對(duì)其進(jìn)行結(jié)構(gòu)確證。采用LPS誘導(dǎo)的小鼠巨噬細(xì)胞RAW264.7炎癥模型，通過Griess法測(cè)定細(xì)胞培養(yǎng)液中NO的釋放量，ELISA法測(cè)定細(xì)胞培養(yǎng)液中IL-6和IL-1β的量以評(píng)價(jià)化合物的體外抗炎活性。結(jié)果 共合成了10個(gè)目標(biāo)化合物，均通過ESI-MS、¹H-NMR及¹³C-NMR對(duì)其結(jié)構(gòu)進(jìn)行確證。體外抗炎活性測(cè)定結(jié)果表明，化合物3d在25 μmol/L時(shí)對(duì)IL-1β的抑制率達(dá)63.96%，對(duì)IL-6的抑制率達(dá)60.99%，與陽性對(duì)照藥塞來昔布活性相當(dāng)。結(jié)論 4-烷氧甲酰基苯并（口惡）唑酮類化合物可通過抑制NO、IL-6和IL-1β炎癥因子的釋放而發(fā)揮抗炎活性。

Objective To design and synthesize 4-alkyloxycarbonyl-benzoxazolone compounds, and to study their anti-inflammatory activity in vitro. Methods 3-Hydroxy-2-amino benzoic acid was used as the starting material to gain a series of target compounds through esterification, cyclization, and substitution reaction, and their structures were confirmed. Subsequently, all of the synthesized compounds were incubated with lipopolysaccharide (LPS) induced rat macrophage RAW264.7 cell, then the expression of NO, IL-1β, and IL-6 were determined by Griess and ELISA assays kits to evaluate the anti-inflammatory activity in vitro. Results Ten benzoxazolone compounds were synthesized, and the structures were characterized by ESI-MS, ¹H-NMR, and ¹³C-NMR. The anti-inflammatory activity assays showed that compound 3d had good inhibitory activity against IL-1β and IL-6 with inhibition rate of 63.96% and 60.99%, and it was near to that of the control drug celecoxib. Conclusion 4-Alkyloxycarbonyl-benzoxazolone compounds exhibit anti-inflammatory activity by inhibiting the expression of NO, IL-6 and IL-1β.

國家自然科學(xué)基金資助項(xiàng)目（81602976）；山西省青年科技研究基金（201601D021159）；山西省回國留學(xué)人員重點(diǎn)科研資助項(xiàng)目（2014-重點(diǎn)2）；山西省高等學(xué)?？萍紕?chuàng)新項(xiàng)目（2014132、2015150）；山西醫(yī)科大學(xué)博士啟動(dòng)金（03201319）