Beta-carbonyl substituted glutathione conjugates as inhibitors Of O. volvulus GST2

P M Brophy; A M Campbell; A J van Eldik; P H Teesdale-Spittle; E Liebau; M F Wang

doi:10.1016/s0960-894x(00)00142-6

Beta-carbonyl substituted glutathione conjugates as inhibitors Of O. volvulus GST2

Bioorg Med Chem Lett. 2000 May 1;10(9):979-81. doi: 10.1016/s0960-894x(00)00142-6.

Authors

P M Brophy¹, A M Campbell, A J van Eldik, P H Teesdale-Spittle, E Liebau, M F Wang

Affiliation

¹ Institute of Biological Sciences, University of Wales, Ceredigion, UK.

PMID: 10853673
DOI: 10.1016/s0960-894x(00)00142-6

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Filaricides / chemical synthesis*
Filaricides / pharmacology
Glutathione / analogs & derivatives*
Glutathione / chemical synthesis*
Glutathione / pharmacology
Glutathione Transferase / antagonists & inhibitors*
Indicators and Reagents
Onchocerca volvulus / drug effects
Onchocerca volvulus / enzymology*
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Filaricides
Indicators and Reagents
Glutathione Transferase
Glutathione