哒嗪酮类α_1-肾上腺素受体拮抗剂的合成和生物活性研究  

Studies on Synthesis and Biological Activity of Pyridazinone Derivatives as α_1-Adrenoceptor Antagonist

作　　者：习保民[1] 江振洲[2] 王涛[2] 倪沛州[3] 

机构地区：[1]中国药科大学物理化学教研室,南京210038 [2]中国药科大学新药筛选中心,南京210038 [3]中国药科大学有机化学教研室,南京210038

出　　处：《有机化学》2006年第11期1576-1583,共8页Chinese Journal of Organic Chemistry

基　　金：863计划(No.2002AA223118);中国药科大学青年基金(No.D0322)资助项目.

摘　　要：将苯(氧)乙胺和苯氧烷胺类α1-肾上腺素受体拮抗剂中的苯(氧)乙胺、苯氧烷胺片段引入哒嗪酮类化合物中,设计、合成了30个新的含哒嗪酮环的α1-肾上腺素受体拮抗剂．所有新化合物的结构均经1H NMR,IR,HRMS确证．生物活性测试表明28个目标物对α1-肾上腺素受体有较好的拮抗作用(pA2>6．00),化合物6o,6p,6q,6v,6x,6y,10c,10d的pA2值>7．00．Phenylethylamine and phenoxylalkylamine fragments were introduced into pyridazinone derivatives （as α1-adrenoceptor antagonist） for the fh-st time. 30 new compounds of pyridazinone were designed and synthesized. The structures of the new compounds were identified by 1H NMR, IR and HRMS spectra. Target compounds have been assayed with function analysis in anococcyeus muscle. The results indicate that 28 target compounds have good blocking activity to α1-adrenoceptor （pA2〉6.00）, The pA2 of compounds 6o, 6p, 6q, 6v, 6x, 6y, 10c and 10d were beyond 7.00.

关 键 词：哒嗪酮 合成 生物活性 α1-肾上腺素受体拮抗剂 

分 类 号：R914[医药卫生—药物化学]