新型前列腺素生成酶抑制剂的研究  

Studies on Novel Prostaglandin Synthetase Inhibitors

作　　者：吴太文[1] 丁惟培[1] 司远征[2] 吴熙瑞[2] 

机构地区：[1]同济医科大学药学系 [2]同济医科大学生殖医学中心

出　　处：《同济医科大学学报》1991年第2期77-80,共4页Acta Universitatis Medicinae Tongji

摘　　要：以各种二苯甲酮或苯甲醛与各种苯乙腈类缩合,合成了16个三苯丙烯腈或二苯丙烯腈类衍生物,应用牛精囊腺微粒体酶温育和PG放射免疫分析方法,检验了这些化合物的活性,结果表明二苯丙烯腈类衍生物的活性强于三苯丙烯腈类衍生物,给电子官能团的二苯丙烯腈类活性强于吸电子官能团的衍生物,其中9号化合物的活性较萘普生强一个多数量级。三苯丙烯腈类化合物和二苯丙烯腈类化合物中分别有几个做了X-ray分析。16 Triphenylacrylonitriles or Diphenylacrylonitriles have been synthesized by condensing various benzophenones or benzaldhydes with various phenylacetonitriles. The pharmacological potency of these compounds were studied by the incubation of bovine seminal vesicle microsomes and PG-RIA. The results show that the potency of inhibition of PG biosynthetase of Diphenylacrylonitriles was stronger than that of Triphenylacrylonitriles. Compounds with electron-releasing function groups proved to be more effective than those with electron-attracting function groups.Compound DPE-g was the most active one, the potency of which was 40 times stronger than that of naproxen. The structure of some compounds has been analysed by X-ray differaction. In addition, the relationship between structure and activity was also investigated by means of X-ray differaction, UV and NMR.

关 键 词：PGSI 三苯丙烯腈类 二工本丙烯腈类 

分 类 号：R965.3[医药卫生—药理学]