NSAIDs-贝母素乙酯的合成与药理活性评价

Synthesis and in vivo efficacy evaluation of NSAIDs-verticinone esters

目的:研究NSAID-贝母素乙酯的合成方法,评价其镇咳、抗炎、平喘的药理活性。方法:分别用4种NSAID药物与贝母素乙通过酯化反应得到目标化合物。通过小鼠镇咳实验、小鼠耳肿胀实验以及豚鼠平喘实验,考察其镇咳、抗炎、平喘活性。结果:成功合成4种化合物,并完成其结构鉴定。化合物3,4,5呈现出较好的镇咳活性,并能显著延长咳嗽潜伏期;化合物2,3,5的抗炎效果显著;4种化合物均有一定的平喘活性。结论:4种NSAID-贝母素乙酯都在不同程度上保留或增强了其原料药物的镇咳、抗炎、平喘药理活性,为进行进一步研究奠定了基础。

Objective：To synthesize non-steroidal anti-inflammatory drugs（NSAIDs）-verticinone esters and evaluate their efficacies in vivo.Methods：Four new compounds were synthesized by ester linkages between NSAIDs（dexibuprofen,indomethacin,dexketoprofen,naproxen） and verticinone based on twin drug theory.The antitussive,anti-inflammatory and anti-asthmatic activities of these new compounds were evaluated.Results：The 4compounds were successfully synthesized and their structures were identified.Compounds 3,4 and 5 had an antitussive activity,prolonged latency period of cough and obviously inhibited cough.Compounds 2,3 and 5 showed a significant anti-inflammatory activity.All these compounds had a potential anti-asthmatic activity.Compounds 3and 5 had a better pharmacological activity than others.Conclusion：The NSAIDs-verticinone esters show the original activities of NSAIDs and verticinone and also enhance their activities,providing a basis for further studies.