β-Carbonyl substituted glutathione conjugates as inhibitors of O. volvulus GST2

…, AJ van Eldik, PH Teesdale-Spittle, E Liebau…

Index: Brophy, Peter M.; Campbell, Alison M.; Van Eldik, Annamaria J.; Teesdale-Spittle, Paul H.; Liebau, Eva; Wang, Meng F. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 9 p. 979 - 981

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Citation Number: 21

Abstract

A series of β-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 πGST. Inhibition of OvGST2 has been demonstrated at low micromolar concentrations for these conjugates and selectivity for OvGST2 over human π-GST of greater than 10-fold has been achieved.