吡里酮二甲醇酯类化合物的合成及其抗炎镇痛活性

目的为探讨吡里酮类化合物抗炎镇痛作用的构效关系,设计合成了吡里酮二甲醇的单酯和二酯类化合物,并进行抗炎及镇痛活性试验.方法采用羟醛缩合反应和酯化反应合成目标化合物,以小鼠耳肿胀法和醋酸扭体法分别测定目标化合物的抗炎和镇痛活性.结果与结论合成得到了10个目标化合物(均未见文献报道),其结构经IR、1H-NMR、MS确定.药理实验表明,目标化合物均具有一定的抗炎或镇痛作用.

Synthesis of esters of pyrrolizinonedimethanol and their anti-inflammatory and analgesia activities

Aim To search the SAR of anti-inflammatory and analgesic of pyrrolizinones, the monoesters and diesters of pyrrolizinonedimethanol were designed and synthesized. Methods The target compounds were synthesized via Aldol condensation and esterification. The anti-inflammatory and analgesic activities were tested on xylene-induced mouse ear edema and acetic acid-induced mouse writhing. Result Ten new target compounds were synthesized. Their chemical structures were confirmed by IR, XH-NMR, and MS and their pharmacological activities were tested. Conclusion Most of them exhibit the good anti-inflammatory activities and/or analgesia activities, and one compound shows more potent anti-inflammatory activity than ibuprofen.