吡里酮类化合物的合成及抗炎镇痛活性研究

Synthesis and anti-inflammatory/analgesia activities of pyrrolizinones

目的寻找高效低毒的具有抗炎镇痛作用的吡里酮类化合物。方法将NO供体的研究与吡里酮类化合物的研究相结合,设计合成NO释放型吡里酮衍生物。其结构经IR1、H-NMR、MS确证。以小鼠耳肿胀法和醋酸扭体法分别测定了目标化合物的抗炎和镇痛活性。结果与结论合成了15个NO释放型吡里酮类化合物,均为未见文献报道的新化合物。部分化合物具有较强的抗炎作用或镇痛作用。

Aim To search the pyrrolizinones derivatives with high anti-inflammatory and analgesic activities and lower side-effect. Methods Combining the result of NO donor research with pyrrolizinone research, some derivatives of 3H-1, 2-dihydro-1-pyrrolizinones having NO-releasing function were designed and synthesized. Their chemical structures were confirmed by IR, ^1H-NMR, and MS. The anti-inflammatory and analgesic activities were tested on xylene-induced mouse ear edema and acetic acid-induced mouse writhing. Result and conclusion Fifteen pyrrolizinone derivetives were prepared. None of them has been reported before. The preliminary pharmacological tests show some of them exhibit the anti-inflammatory activities and/or analgesia activities.