TY - JOUR
T1 - 2-Amino-4-{3'-hydroxyphenyl]-4-hydroxybutanoic Acid; A Potent Inhibitor of Rat and Recombinant Human Kynureninase
AU - Walsh, HA
AU - Leslie, PL
AU - O'Shea, KC
AU - Botting, Nigel Peter
PY - 2002/2/11
Y1 - 2002/2/11
N2 - 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.
AB - 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.
KW - CYSTEINE S,S-DIOXIDES
UR - http://www.scopus.com/inward/record.url?scp=0037059896&partnerID=8YFLogxK
UR - http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6TF9-44YVWXR-7&_user=1026342&_coverDate=02%2F11%2F2002&_alid=178383236&_rdoc=16&_fmt=full&_orig=search&_cdi=5221&_sort=d&_st=4&_docanchor=&_acct=C000050565&_version=1&_urlVersion=0&_userid=1026342&md5=6da7dcff327272ff9773d4ae2ce760eb
M3 - Article
VL - 12
SP - 361
EP - 363
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 3
ER -