3-p(ε—取代氨基烃氧基)苯甲酰吲哚衍生物的镇痛和抗电休克活性

摘要: 5-羟色胺是吲哚类脑内神经递质,参与脑内痛觉的调节。我们曾证实次甲二氧-3-(1-β-乙基-4-甲基哌嗪)吲哚衍生物有较强的抗电休克及镇痛活性。在吲哚母核的2位氢以甲基、苯基取代或不取代,得3个系列衍生物;在吲哚母核3位上带有碱性醚链的末端氨基氮上,以不同基团取代,共得21个化合物。本文对这些化合物进行了镇痛及抗电休克活性的筛选,并对它们进行了构效关系的分析。

Abstract: Three series of indole derivatives were tested for their anticonvulsant(electric shock method)and analgesic(hot plate method)activities in mice. Compounds with a benzne ring attached to 2 position of Indole nucleus and with subsitution of two CH_3 or C_2H