Synthesis and pharmacology of new enantiopure Δ3-4-arylkainoids

被引：21

作者：

Rondeau, D

Gill, P

Chan, M

Curry, K

Lubell, WD

机构：

[1] Univ Montreal, Dept Chim, Montreal, PQ H3C 3J7, Canada

[2] IGT Pharma Inc, CNS Res Div, Vancouver, BC V6T 1Z3, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)00093-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Seven Delta(3)-4-arylkainoids possessing various 4-position aromatic and heteroaromatic groups were synthesized and their apparent affinities were measured in order to explore the influences of 4-position electron density and stereochemistry on receptor affinity and specificity. Kainoids 1a-f were shown to be selective agonists at the NMDA receptor and the electron rich furanyl and thienyl analogues exhibited the highest affinities. Naphthylkainoid 1g proved to be a nonselective antagonist at the iGluRs. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：771 / 773

页数：3

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