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一类在C-7位带有取代苯基的新型喹喔啉羧酸的合成及其AMPA受体拮抗活性

Synthesis and AMPA receptor antagonistic activity of a novel class of quinoxalinecarboxylic acid with a substituted phenyl group at the C-7 position.

作者信息

Takano Yasuo, Shiga Futoshi, Asano Jun, Ando Naoki, Uchiki Hideharu, Anraku Tsuyosi

机构信息

Discovery Research Laboratories, Kyorin Pharmaceutical Co., Ltd., 2399-1, Nogi, Nogi-machi, Simotsuga-gun, Tochigi 329-0114, Japan.

出版信息

Bioorg Med Chem Lett. 2003 Oct 20;13(20):3521-5. doi: 10.1016/s0960-894x(03)00740-6.

Abstract

The synthesis and biological properties of a novel class of 7-heterocycle-substituted quinoxalinecarboxylic acids, which bear a substituted phenyl group through a urethane linkage at the C-7 position, are described. One of the synthesized compounds, 15l, which has a 4-carboxyphenyl carbamoyloxymethyl imidazole group at the C-7 position and is water-soluble, was found to possess high potency in vitro and showed excellent neuroprotective efficacy in vivo.

摘要

描述了一类新型的7-杂环取代喹喔啉羧酸的合成及其生物学性质,这类化合物在C-7位通过氨基甲酸酯键连接一个取代苯基。所合成的化合物之一15l,在C-7位具有4-羧基苯基氨基甲酰氧基甲基咪唑基团且可溶于水,被发现具有高效的体外活性,并在体内显示出优异的神经保护功效。

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