四氢吡啶并1,2-a吲哚类化合物的合成及其扩张脑血管活性

SYNTHESIS AND CEREBRAL VASODILATING EFFECTS OF TETRAHYDRO-PYRIDO 1,2-a INDOLE DERIVATIVES

摘要: 本文报道了7个2-取代-6-氧代-10-2-(N-取代)氨甲酰基乙基-6,7,8,9-四氢吡啶并1,2-a吲哚类化合物的合成。初步药理试验表明,设计合成的化合物均有一定程度的扩张脑血管作用,其中化合物Ⅰ₇的作用最为明显。构效关系显示酰胺结构中二乙氨基乙胺的作用强于二甲氨基乙胺。

Abstract: Aseries of 2-substituted-6-oxo -10 -2-(N- substituted)carbamoyl ethyl -6,7,8,9-tetrahydro-pyrido1,2 -a indole compounds were synthesized for studying the relation between structures and cerebrovascular activities. The structures of compounds synthesized were confirmed by means of ¹HNMR, M S, IR, UV and elemental analysis.Preliminary pharmacological experiments showed that all these new compounds were effective for cerebral vasodilation. Compound I₇ was the best of all. The β- diethylaminoethylamine moiety seems to be better than β- dimethylaminoethylamine.