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.
引用
收藏
页码:257 / 265
页数:9
相关论文
共 24 条
  • [21] SYNTHESIS OF OXYSANGUINARINE
    SHAMMA, M
    TOMLINSON, HH
    [J]. JOURNAL OF ORGANIC CHEMISTRY, 1978, 43 (14) : 2852 - 2855
  • [22] BLOCKADE OF N-METHYL-D-ASPARTATE RECEPTORS MAY PROTECT AGAINST ISCHEMIC DAMAGE IN THE BRAIN
    SIMON, RP
    SWAN, JH
    GRIFFITHS, T
    MELDRUM, BS
    [J]. SCIENCE, 1984, 226 (4676) : 850 - 852
  • [23] THIOLLAIS R, 1947, B SOC CHIM FR, P708
  • [24] VAULTIER M, 1986, B SOC CHIM FR, P83