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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Authors
Dou, Dengfeng
Viwanathan, Prasanth
Li, Yi
He, Guijia
Alliston, Kevin R.
Lushington, Gerald H.
Brown-Clay, Joshua D.
Padmanabhan, Radhakrishnan
Groutas, William C.
Advisors
Issue Date
2010-11-08
Type
Article
Keywords
Research Support, N.I.H., Extramural
Research Projects
Organizational Units
Journal Issue
Citation
Journal of combinatorial chemistry. 2010 Nov 8; 12(6): 836-43.
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 led 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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Description
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Publisher
American Chemical Society
Journal
Book Title
Series
Journal of combinatorial chemistry
J Comb Chem
PubMed ID
DOI
ISSN
1520-4774
EISSN