Beta-carbonyl substituted glutathione conjugates as inhibitors Of O. volvulus GST2.
A series of beta-carbonyl substituted glutathione conjugates were prepared and evaluated as inhibitors of OvGST2. Their specificity for the parasite derived protein was assessed through comparison with their inhibition of human piGST. Inhibition of OvGST2 has been demonstrated at low micromolar concentrations for these conjugates and selectivity for OvGST2 over human pi-GST of greater than 10-fold has been achieved.
Brophy
P M
PM
Institute of Biological Sciences, University of Wales, Ceredigion, UK.
Campbell
A M
AM
van Eldik
A J
AJ
Teesdale-Spittle
P H
PH
Liebau
E
E
Wang
M F
MF
D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D005369:Filaricides / Q000138:chemical synthesis* / Q000494:pharmacology; D005978:Glutathione / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D005982:Glutathione Transferase / Q000037:antagonists & inhibitors*; D007202:Indicators and Reagents; D017181:Onchocerca volvulus / Q000187:drug effects / Q000201:enzymology*; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D005369:Filaricides; D007202:Indicators and Reagents; D005982:Glutathione Transferase; D005978:Glutathione