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[3-羧基-4-苯基异喹啉衍生物的氨基和二烷基氨基链烷酰胺的合成及药理活性。I]

[Synthesis and pharmacological activity of amino- and dialkylaminoalkamides of derivatives of 3-carboxy-4-phenylisoquinoline. I].

作者信息

Duro F, Santagati N A, Vittorio F

出版信息

Farmaco Sci. 1981 Jun;36(6):400-11.

PMID:6974099
Abstract

The synthesis of a series of 1-amino derivatives of 3-carboxymethyl-4-phenylisoquinoline and of dialkylaminoalkylamides of 2-methyl-3-carboxy-4-phenyl-1,2-dihydro-1-oxoisoquinoline and of 1-methoxy-3-carboxy-4-phenylisoquinoline is described. The pharmacological activity of some of these compounds was studied. 1-Morpholino-3-carboxymethyl-4-phenylisoquinoline (IV a) and 1-pyrrolidino derivatives (IV d) caused reduction in spontaneous activity and reactivity in mice whereas compounds (VIII a) and (XII b) showed good local anesthetic activity in infiltration tests.

摘要

本文描述了一系列3-羧甲基-4-苯基异喹啉的1-氨基衍生物、2-甲基-3-羧基-4-苯基-1,2-二氢-1-氧代异喹啉的二烷基氨基烷基酰胺以及1-甲氧基-3-羧基-4-苯基异喹啉的合成。研究了其中一些化合物的药理活性。1-吗啉代-3-羧甲基-4-苯基异喹啉(IV a)和1-吡咯烷基衍生物(IV d)可降低小鼠的自发活动和反应性,而化合物(VIII a)和(XII b)在浸润试验中显示出良好的局部麻醉活性。

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