8-氨甲基取代木犀草素衍生物的合成和抗炎活性研究

Synthesis of derivatives of 8-aminomethylluteolin and their anti-inflammatory activity

以木犀草素为先导化合物,对其A环8-位碳上进行Mannich反应,合成了10个未见文献报道的8-氨甲基化衍生物,并用1HNMR,IR和MS(HRMS)进行了结构表征。利用二甲苯诱发小鼠耳廓肿胀模型对所合成的七个目标化合物进行了抗炎活性的药理筛选,初步结果表明部分化合物具有良好的抗炎活性。

Ten new aminomethylation products were synthesized at C - 8 in A - ring via Mannich reaction with luteolin as leading compound. All these new derivatives were identified by IR, i H NMR and MS （ HRMS ）. Seven targeting compounds have been examined about their anti - inflammatory activity on xylene induced mice edema and the preliminary bioassay suggests that some of them exhibited potential anti - inflammatory activity.