2-苯基-四氢噻喃并嘧啶类化合物的合成及黄嘌呤氧化酶抑制活性  

Synthesis and xanthine oxidase inhibitory activities of 2-phenyl-tetrahydrothiopyrano[4,3-d] pyrimidine derivatives

作　　者：李晶[1] 任月娇[1] 关溯[1] 张雷[1] 

机构地区：[1]华南理工大学生物科学与工程学院,广州510006

出　　处：《中国药科大学学报》2015年第3期294-300,共7页Journal of China Pharmaceutical University

基　　金：广东省自然科学基金资助项目(No.S2013010012018)~~

摘　　要：以4-羟基苯甲腈为原料,经醚化、水解、酰化、加成等反应,共合成12个新型的2-苯基-四氢噻喃并嘧啶类化合物(6a^6d,8a^8h),并进行抑制黄嘌呤氧化酶活性测试。结果表明:化合物8a^8h(100μmol/L)均表现出不同程度的抑酶活性,其活性明显强于化合物6a^6d,即嘧啶环上引入羧基有利于提高抑酶活性;在化合物8a^8h中,以嘧啶环上异丙酸取代,苯环羟基乙醚化的8f活性最强,IC50为76.0μmol/L。Twelve novel 2-phenyl -tetrahydrothiopyrano [ 4, 3-d] pyrimidine derivatives were synthesized from 4-hydroxy-benzonitrile by etherification, hydrolysis, acylation and addition reactions, etc. The inhibitory activities against xanthine oxidase were evaluated in vitro. Results showed that compounds 8a-Sh exhibited varying inhibitory potencies on xanthine oxidase at 100 ixmol/L, significantly better than those of compounds 6a-6d, indicating that carboxy-substituted pyrimidine is beneficial to the inhibitory activity. Among compounds 8a-Sh, 8f with isopropi- onic acid-substituted pyrimidine and ethyl-substituted phenol showed the best inhibition with IC50 of 76. 0 μmol/L.

关 键 词：四氢噻喃 嘧啶 合成 黄嘌呤氧化酶抑制剂 抑制活性 

分 类 号：R914.5[医药卫生—药物化学]