Modulators of the kynurenine pathway of tryptophan metabolism:: Synthesis and preliminary biological evaluation of (S)-4-(ethylsulfonyl)benzoylaianine, a potent and selective kynurenine aminotransferase II (KAT II) inhibitor

被引：69

作者：

Pellicciari, Roberto ^{[1
]}

Rizzo, Rosa C. ^{[1
]}

Costantino, Gabriele ^{[1
]}

Marinozzi, Maura ^{[1
]}

Amori, Laura ^{[1
]}

Guidetti, Paolo ^{[1
]}

Wu, Hui-Qiu ^{[1
]}

Schwarcz, Robert ^{[1
]}

机构：

[1] Univ Perugia, Dipartimento Chim & Tecnol Farmaco, I-06123 Perugia, Italy

来源：

CHEMMEDCHEM | 2006年 / 1卷 / 05期

关键词：

Enzymes; Kynurenic acid; Kynurenine aminotransferase II; Kynurenine pathway; Medicinal chemistry;

D O I：

10.1002/cmdc.200500095

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(S)-4-(Ethylsulfonyl)benzoylalanine is a potent and selective inhibitor of kynurenine aminotransferase II (KAT II) with no significant effect on KAT I or other enzymes of the kynurenine pathway. This compound is able to pronouncedly inhibit the formation of kynurenic acid (KYNA) in rat brain.

引用

页码：528 / +

页数：5

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