摘要
以吲哚嗪类化合物Ｂｕｔｏｐｒｉｚｉｎｅ为先导物，结合β－受体阻断剂的结构特点，设计合成了９个吲哚嗪类化合物，均未见文献报道，其化学结构经红外光谱、核磁共振、质谱和元素分析确证。抗氯仿诱发小鼠室颤结果表明，化合物(２)，(６)具有明显的抗心律失常活性。
Nine 2-ethyl-3-[4-(2-hydroxyl-3-alkylaminopropanoxyl)benzoyl]indolizines(alkyl=iso-pr,n-butyl,iso-butyl,tert-butyl,diethyl,benzyl ,cyclopentyl,3,4-dimethoxyphenethyl,3,4-methylenedoxyphenethyl )compounds were prepared. The screening tests of the(9)compounds indicated that(2)(R=tert-butyl )and(6)(R=3,4-dimethoxyphenethyl)could markedly antagonize CHCI3-induced arrhythmia in mice。Thus,2-picoline was treated with ClCH2CO2Et and cyclized with(EtCO)2O,2-ethylindolizine treated with4-(4--MeC6H4SO3)C6H4COCl,2-ethyl-3-( 4-tosyloxybenzoyl )indolizine detosylated,the hydroxybenzoylindolizine treated with epoxy chloropropane and tert-butylamine to give(2),which could antagonize 80%of CHCl3-induced arrhythmias in mice.
出处
《中国药物化学杂志》
CAS
CSCD
1994年第3期157-161,170,共6页
Chinese Journal of Medicinal Chemistry
