SYNTHESIS OF NOVEL ISOQUINOLINE DERIVATIVES AS POTENTIAL CNS-AGENTS

被引：34

作者：

BONNAUD, B

CARLESSI, A

BIGG, DCH

机构：

[1] Centre de Recherche Pierre Fabre, Castres, F-81106

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 1993年 / 30卷 / 01期

关键词：

D O I：

10.1002/jhet.5570300144

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of 4-aminomethyl-1,2,3,4-tetrahydroisoquinoline derivatives were prepared as potential CNS-agents acting via amino-acid neurotransmitter systems. The compounds were synthesized from 1,2,3,4-tetra-hydro-1-oxoisoquinoline-4-carboxylic acids obtained by dipolar cycloadditon reactions of imines with homophthalic anhydride. Among the compounds testes 5c and 5m showed sub-micromolar affinity for the NMDA receptor and represent a structurally novel class of ligand for this site.

引用

页码：257 / 265

页数：9

共 24 条

[1] A STUDY AND MECHANISTIC INTERPRETATION OF THE ELECTRONIC AND STERIC EFFECTS THAT DETERMINE THE STEREOCHEMICAL OUTCOME OF THE REACTION OF SCHIFF-BASES WITH HOMOPHTHALIC ANHYDRIDE AND 3-PHENYLSUCCINIC ANHYDRIDE [J].