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Sanjay Samanta, Dr. Taian Cui and Prof. Yulin Lam Discovery, Synthesis, and in vitro Evaluation of West Nile Virus Protease Inhibitors Based on the 9,10-Dihydro-3H,4aH-1,3,9,10a-tetraazaphenanthren-4-one Scaffold ChemMedChem 7

Article first published online: 30 APR 2012 | DOI: 10.1002/cmdc.201200136

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Running cofactor interference: In vitro assays with West Nile virus (WNV) NS2B–NS3 protease resulted in the discovery of 9,10-dihydro-3H,4aH-1,3,9,10a-tetraazaphenanthren-4-ones as a new class of inhibitors of this enzyme. Optimization of the lead compound led to an uncompetitive WNV NS2B–NS3 inhibitor with an IC50 value of 5.41±0.45 μM.

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