The conjugates obtained by the combination of indole and aminophenyl morpholinone were screened for TNF-α and IL-6 inhibition in microglial cells. Compound 4 was found to be the most potent anti-inflammatory agent as it reduced LPS induced level of inflammatory cytokines TNF-α and IL-6 by 71% and 53%, respectively. A significant decrease in NO and MMPs release from BV2 cells in culture pretreated with this compound as well as inhibition of nuclear translocation of NF-κB and AP-1 was observed. 75% inhibition of acetic acid induced algesia in swiss albino mice was noticed in the presence of compound 4. Experimental data and molecular docking studies indicate that the compounds are targeting TNF-α, iNOS and IL-6.

筛选由吲哚和氨基苯基吗啉酮组合获得的缀合物在小胶质细胞中的TNF-α和IL-6抑制作用。发现化合物4是最有效的抗炎剂，因为其将LPS诱导的炎性细胞因子TNF-α和IL-6的水平分别降低了71％和53％。在用该化合物预处理的培养物中，从BV2细胞释放的NO和MMP明显减少，并且抑制了NF-κB和AP-1的核转运。在化合物4的存在下，观察到瑞士白化病小鼠中乙酸诱导的痛觉过敏的抑制率为75％。实验数据和分子对接研究表明这些化合物靶向TNF-α，iNOS和IL-6。