Design, Synthesis and In Vitro Evaluation of Potential West Nile Virus Protease Inhibitors Based on the 1-Oxo-1, 2, 3, 4- tetrahydroisoquinoline and 1-Oxo-1, 2-dihydroisoquinoline Scaffolds

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Issue Date
2010-11Author
Dou, Dengfeng
Viwanathan, Prasanth
Li, Yi
He, Guijia
Alliston, Kevin R.
Lushington, Gerald H.
Brown-Clay, Joshua D.
Padmanabhan, Radhakrishnan
Groutas, William C.
Publisher
American Chemical Society
Type
Article
Article Version
Scholarly/refereed, author accepted manuscript
Rights
Copyright © American Chemical Society
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Show full item recordAbstract
The 1-Oxo-1, 2, 3, 4-tetrahydroisoquinoline and 1-Oxo-1, 2-dihydroisoquinoline scaffolds were utilized in the design and solution phase synthesis of focused libraries of compounds for screening against West Nile Virus (WNV) protease. Exploratory studies have lead to the identification of a WNV protease inhibitor (a 1-oxo-1, 2-dihydroisoquinoline-based derivative, 12j) which could potentially serve as a launching pad for a hit-to-lead optimization campaign. The identified hit was devoid of any inhibitory activity toward a panel of mammalian serine proteases.
Description
This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Combinatorial Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://doi.org/10.1021/cc100091h.
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Citation
Dou, D., Viwanathan, P., Li, Y., He, G., Alliston, K. R., Lushington, G. H., … Groutas, W. C. (2010). Design, Synthesis and In Vitro Evaluation of Potential West Nile Virus Protease Inhibitors Based on the 1-Oxo-1, 2, 3, 4-tetrahydroisoquinoline and 1-Oxo-1, 2-dihydroisoquinoline Scaffolds. Journal of Combinatorial Chemistry, 12(6), 836–843. http://doi.org/10.1021/cc100091h
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