beta-carbonyl substituted glutathione conjugates as inhibitors of O-volvulus GST2

Authors
Brophy, PM Campbell, AM van Eldik, AJ Teesdale-Spittle, PH Liebau, E Wang, MF
Citation
Pm. Brophy et al., beta-carbonyl substituted glutathione conjugates as inhibitors of O-volvulus GST2, BIOORG MED, 10(9), 2000, pp. 979-981
Citations number
7
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
9
Year of publication
2000
Pages
979 - 981
Database
ISI
SICI code
0960-894X(20000501)10:9<979:BSGCAI>2.0.ZU;2-5
Abstract
A series of beta-carbonyl substituted glutathione conjugates were prepared and evaluated as inhibitors of OvGST2. Their specificity for the parasite d erived protein was assessed through comparison with their inhibition of hum an pi GST. Inhibition of OvGST2 has been demonstrated at low micromolar con centrations for these conjugates and selectivity for OvGST2 over human pi-G ST of greater than 10-fold has been achieved. (C) 2000 Elsevier Science Ltd . All rights reserved.