The role of the side chain in determining relative δ- and κ-affinity in C5′-substituted analogues of naltrindole

被引：16

作者：

Black, SL

Jales, AR

Brandt, W

Lewis, JW

Husbands, SM ^{[1
]}

机构：

[1] Univ Bath, Dept Pharm, Bath BA2 7AY, Avon, England

[2] Univ Bath, Dept Pharmacol, Bath BA2 7AY, Avon, England

[3] Univ Bristol, Sch Chem, Bristol BS8 1TS, Avon, England

[4] Inst Plant Biochem, D-06120 Halle An Der Saale, Germany

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 02期

关键词：

D O I：

10.1021/jm020997b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The role of the side chain in 5'-substituted analogues of naltrindole has been further explored with the synthesis of series of amides, amidines, and ureas. Amidines (8, 13) had greatest selectivity for the kappa receptor, as predicted from consideration of the message-address concept. It was also found that an appropriately located carbonyl group, in ureas (10) and amides (7), led to retention of affinity and antagonist potency at the 6 receptor.

引用

页码：314 / 317

页数：4

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