摘要
以吲哚嗪类化合物Ｂｕｔｏｐｒｏｚｉｎｅ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，其化学结构经红外光谱、核磁共振、质谱和元素分析证实。对抗氯仿诱发小鼠室颤结果表明，化合物Ⅱ２、Ⅱ６具有明显的抗心律失常活性。
Nine compounds of 2-ethyl-3-[4-(2-hydroxyl-3-alkylaminopropanoxyl) benzoyl] indolizines (alkyl=iso-Pr, n-butyl, iso-butyl, tertbutyl, diethyl, benzyl, cyclopentyl, 3, 4-dimethoxyphenethyl, 3,4-methylenedoxyphenethyl) were prepared.Screening test of 9 compounds indicated that Ⅱ2 (R=tert-butyl) and Ⅱ6(R=3, 4-dimethoxyphenethyl) could markedly antagonize CHCl3-induced arrhythmia in rats.Thus, 2-picoline was treated with ClCH2CO2Et and cyclized with (EtCO)2O, 2-ethylindolizine treated with 4-(4-MeC6H4SO3) C6H4COCl,2-ethyl-3-(4-tosyloxybenzoyl)indolizine detosylated, the hydroxybenzoylindolizine treated with epoxy chloropropane and tert-butylamine to give Ⅱ2, Which could antagonize 80% CHCl3 induced arrhythmias in rats.
出处
《山东医科大学学报》
1994年第4期338-342,共5页
Acta Academiae Medicinae Shandong
