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Bioorg Med Chem. 2012 Feb 1;20(3):1213-21. doi: 10.1016/j.bmc.2011.12.047. Epub 2011 Dec 30.

Inhibition of Dengue virus and West Nile virus proteases by click chemistry-derived benz[d]isothiazol-3(2H)-one derivatives.

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  • 1Department of Chemistry, Wichita State University, Wichita, KS 67260, USA.


Two click chemistry-derived focused libraries based on the benz[d]isothiazol-3(2H)-one scaffold were synthesized and screened against Dengue virus and West Nile virus NS2B-NS3 proteases. Several compounds (4l, 7j-n) displayed noteworthy inhibitory activity toward Dengue virus NS2B-NS3 protease in the absence and presence of added detergent. These compounds could potentially serve as a launching pad for a hit-to-lead optimization campaign.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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