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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

Dou, Dengfeng
; 
Viwanathan, Prasanth
; 
Li, Yi
; 
He, Guijia
; 
Alliston, Kevin R.
; 
Lushington, Gerald H.
; 
Brown-Clay, Joshua D.
; 
Padmanabhan, Radhakrishnan
; 
Groutas, William C.
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Abstract
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.
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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.
Date
2010-11
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American Chemical Society
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Chemistry Scholarly Works
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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
URI
https://hdl.handle.net/1808/24258
DOI
10.1021/cc100091h
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