2-Amino-4-{3'-hydroxyphenyl]-4-hydroxybutanoic Acid; A Potent Inhibitor of Rat and Recombinant Human Kynureninase

HA Walsh, PL Leslie, KC O'Shea, Nigel Peter Botting

Research output: Contribution to journalArticlepeer-review

26 Citations (Scopus)

Abstract

A novel structural analogue of kynurenine, 2-amino-4-[3'-hydroxyphenyl]-4-hydroxybutanoic acid 6, was synthesised as an inhibitor of kynureninase. The compound had a significant inhibitory effect on kynureninase from both rat and human, giving a K-i of 100 nM. It was thus found that removal of the aryl amino group coupled with a reduction of the carbonyl group at position 7 of the alanine side chain greatly enhanced potency of the inhibitor. (C) 2002 Elsevier Science Ltd. All rights reserved.

Original languageEnglish
Pages (from-to)361-363
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number3
Publication statusPublished - 11 Feb 2002

Keywords

  • CYSTEINE S,S-DIOXIDES

Fingerprint

Dive into the research topics of '2-Amino-4-{3'-hydroxyphenyl]-4-hydroxybutanoic Acid; A Potent Inhibitor of Rat and Recombinant Human Kynureninase'. Together they form a unique fingerprint.

Cite this