作　　者： ; ; ; ; ;

机构地区： 湖南大学化学化工学院

出　　处： 《化学学报》 2008年第22期2553-2557,共5页

摘　　要： 基于萘普生的构效关系对其羧基进行结构修饰,设计合成了萘普生2-芳基吗啉乙酯类化合物.芳基乙酮经过溴代、胺化、还原得到的2-芳基-4-羟乙基吗啉在三乙胺作缚酸剂存在下与萘普生酰氯反应得到萘普生2-芳基吗啉乙酯类化合物,收率24.2%～76.5%.新化合物结构经1H NMR确认.生物活性实验结果表明:在10μmol/L质量浓度时,化合物1d对COX-2的抑制率达96.32%. The 2-（2-arylmorpholino）ethyl esters of naproxen were designed and synthesized according to the structure-activity relationship by the reaction of 2-aryl-4-（2-hydroxyethyl）morpholine with 2-（6-methoxy-2-naphthyl）propionyl chloride in yields of 24.2%-76.5%. 2-Aryl-4-（2-hydroxylethyl）morpholine intermediates were synthesized from arylethanones by bromination, amination and deoxidization. Their structures were confirmed by ^1H NMR. The preliminary bioassays indicated that compound ld exhibited a 96.32% inhibition rate against COX-2 in vitro at 10μmol/L.

关 键 词： 萘普生 环氧合酶 抑制剂 吗啉衍生物 合成

领　　域： [理学] [理学] [化学工程]