Synthesis and biological evaluation of a series of quinazoline-2-carboxylic acids and quinazoline-2,4-diones as glycine-NMDA antagonists: A pharmacophore model based approach

被引：36

作者：

Colotta, V ^{[1
]}

Catarzi, D ^{[1
]}

Varano, F ^{[1
]}

Cecchi, L ^{[1
]}

Filacchioni, G ^{[1
]}

Galli, A ^{[1
]}

Costagli, C ^{[1
]}

机构：

[1] UNIV FLORENCE,DIPARTIMENTO FARMACOL PRECLIN & CLIN,I-50134 FLORENCE,ITALY

来源：

ARCHIV DER PHARMAZIE | 1997年 / 330卷 / 05期

关键词：

quinazoline-2-carboxylic acids; quinazoline-2,4-diones; glycine-NMDA antagonists;

D O I：

10.1002/ardp.19973300504

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and glycine-NMDA binding activity of a series of quinazoline-2-carboxylic acids 1 and quinazoline-2,4-diones 2, containing all the essential and optional pharmacophoric descriptors by a putative glycine antagonist model, are reported. The binding results show that only three of the title compounds displayed micromolar receptor affinity, demonstrating how disappointing the synthesis of receptor ligands based only on interaction models can be.

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页码：129 / 134

页数：6

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