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Synthesis and evaluation of non-dimeric HCV NS5A inhibitors

Authors :
Amblard, Franck
Zhang, Hongwang
Zhou, Longhu
Shi, Junxing
Bobeck, Drew R.
Nettles, James H.
Chavre, Satish
McBrayer, Tamara R.
Tharnish, Philip
Whitaker, Tony
Coats, Steven J.
Schinazi, Raymond F.
Source :
Bioorganic & Medicinal Chemistry Letters. Apr2013, Vol. 23 Issue 7, p2031-2034. 4p.
Publication Year :
2013

Abstract

Abstract: Based on the symmetrical bidentate structure of the NS5A inhibitor BMS-790052, a series of new monodentate molecules were designed. The synthesis of 36 new non-dimeric NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. Among them compound 5a showed picomolar range activity along with an excellent selectivity index (SI > 90,000). [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
23
Issue :
7
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
86154783
Full Text :
https://doi.org/10.1016/j.bmcl.2013.02.023