Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis

…, H Chakrapani, S Prast-Nielsen, A Jadhav…

Index: Rai, Ganesha; Sayed, Ahmed A.; Lea, Wendy A.; Luecke, Hans F.; Chakrapani, Harinath; Prast-Nielsen, Stefanie; Jadhav, Ajit; Leister, William; Shen, Min; Inglese, James; Austin, Christopher P.; Keefer, Larry; Arner, Elias S. J.; Simeonov, Anton; Maloney, David J.; Williams, David L.; Thomas, Craig J. Journal of Medicinal Chemistry, 2009 , vol. 52, # 20 p. 6474 - 6483

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Citation Number: 53

Abstract

Schistosomiasis is a chronic parasitic disease affecting hundreds of millions of individuals worldwide. Current treatment depends on a single agent, praziquantel, raising concerns of emergence of resistant parasites. Here, we continue our explorations of an oxadiazole-2- oxide class of compounds we recently identified as inhibitors of thioredoxin glutathione reductase (TGR), a selenocysteine-containing flavoenzyme required by the parasite to ...