Inhibitors of Schistosoma mansoni Redox Cascade
SID 11111612
NCGC00015800
Furoxan
Key Investigators
National Center for Advancing Translational Sciences
Ajit Jadhav
Wendy Lea, Ph.D.
David Maloney, Ph.D.
Ganesha Rai, Ph.D.
Anton Simeonov, Ph.D.
Craig Thomas, Ph.D.
Rush University Medical Center
David L. Williams, Ph.D.
Public Health Impact
Schistosomiasis is a debilitating disease affecting approximately 250 million people in more than 70 countries. Current drug treatments are limited, and the parasites causing the disease are becoming resistant to these drugs. This probe compound exhibits anti-schistosomal activity, and serves as a potential lead for anti-schistosomal drug development.
Publications
Lea WA, Jadhav A, Rai G, et al. A 1,536-well-based kinetic HTS assay for inhibitors of Schistosoma mansoni thioredoxin glutathione reductase. Assay Drug Dev Technol, 2008;6:551-555.
Simeonov A, Jadhav A, Sayed AA, et al. Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade. PLoS Negl Trop Dis, 2008;2:1-10; e127.
Sayed AA, Simeonov A, Thomas CJ, et al. Identification of oxadiazoles as new drug leads for the control of schistosomiasis. Nat Med, 2008;14:407-412.
Rai G, Sayed AA, Lea WA, et al. Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis. J Med Chem, 2009;52:6474-6483.
Rai G, Thomas CJ, Leister W, Maloney DJ. Synthesis of oxadiazole-2-oxide analogues as potential antischistosomal agents. Tett Lett, 2009;50:1710-1713.
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