《3,4-二氢-4-(1-哌啶甲基)-5H-1-苯并氧杂-5-酮盐酸盐的合成及其生物活性研究》.pdfVIP

第38卷第4期 精细化工中间体 V01．38No．4 FINECHEMICALINTERMEDIATES 2008 2008年8月 August 合成及其生物活性研究 陈耀，兰惠瑜，孙方，胡春 (沈阳药科大学制药工程学院，辽宁沈阳110016) 摘 酚、y一丁内酯、甲醛和哌啶等原料合成了目标化合物，并利用熔点、红外光谱、核磁共振氢谱等手段确定了其结构。 采用二甲苯致小鼠耳肿胀法．测定了该化合物的抗炎活性。实验结果表明在200mCkg剂量下该化合物对二甲苯所 致小鼠耳肿胀的抑制率为54．5％。采用Borns比浊法测定了该化合物的抗血小板聚集活性，实验结果表明该化合物 的抗jk,J、板聚集活性比噻氯匹啶强约23倍。 关键词：药物化学；环酮；杂环；衍生物；合成；抗炎；抗血小板聚集 中图分类号：R914 文献标识码：A 文章编号：1009—9212(2008)04_0025_03 and SynthesisBiological Activity CHEN Chun Yao，LAN Hui-yu，SUNFang，HU (School 110016，China) of and areknowntoexhibitanti— mannichbasedervatives Abstract：The or，r-unsaturated cyclohexanone cyclopentanone ordertofindsomenew with ketone whichbe toexhibitanti— inflammatoryactivity．In compoundscyclic moiety expected was asthe inflammatory designedtarget were from and asthe compound．Thetargetcompoundsynthesizedphenol，-butyrolactone，formaldehydepiperidine raw characterized and 1HNMR anti— materials，and starting bymeltingpoint，infraredspectraproton spectra．The wasevaluated mouseear model．andthe rateof54．5％atthe inflammatoryactivity usingxylene-inducedswelling inhibitory doseof200 Borns was the method，the evaluated，andinhibitoryactivity ms／ks．Using anti-plateletaggregativeactivity wasabout23timesmore thanthatof