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
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.
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页码:257 / 265
页数:9
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