Synthesis and potent anticonvulsant activities of 4-oxo-imidazo[1,2-a]indeno[1,2-e]pyrazin-8-and-9-carboxylic (acetic) acid AMPA antagonists

被引：13

作者：

Pratt, J ^{[1
]}

Jimonet, P ^{[1
]}

Bohme, GA ^{[1
]}

Boireau, A ^{[1
]}

Damour, D ^{[1
]}

Debono, MW ^{[1
]}

Genevois-Borella, A ^{[1
]}

Randle, JCR ^{[1
]}

Ribeill, Y ^{[1
]}

Stutzmann, JM ^{[1
]}

Vuilhorgne, M ^{[1
]}

Mignani, S ^{[1
]}

机构：

[1] Aventis Pharma SA, Ctr Rech Vitry Alfortville, F-94403 Vitry, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(00)00561-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The over-stimulation of excitatory amino acid receptors such as the glutamate AMPA receptor has been suggested to be associated with neurodegenerative disorders. Here we describe an original series of readily water soluble 4-oxo-imidazo[1,2-a] indeno[1,2-e]pyrazin-8- and -9-carboxylic (acetic) acid derivatives. One of these compounds, 4f, exhibited nanomolar binding affinity, potent competitive antagonism at the ionotropic AMPA receptor and a long duration of anticonvulsant activity after administration by parenteral route in vivo. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2749 / 2754

页数：6

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