Title of article
HCV NS5B polymerase-bound conformation of a soluble sulfonamide inhibitor by 2D transferred NOESY
Author/Authors
Constantin G. Yannopoulos، نويسنده , , Ping Xu، نويسنده , , Feng Ni، نويسنده , , Laval Chan، نويسنده , , Oswy Z. Pereira، نويسنده , , T. Jagadeeswar Reddy، نويسنده , , Sanjoy K. Das، نويسنده , , Carl Poisson، نويسنده , , Nghe Nguyen-Ba، نويسنده , , Nathalie Turcotte، نويسنده , , Melanie Proulx، نويسنده , , Lilianne Halab، نويسنده , , Wuyi Wang، نويسنده , , Jean Bédard، نويسنده , , Nicolas Morin، نويسنده , , Martine Hamel، نويسنده , , Olivier Nicolas، نويسنده , , Darius Bilimoria، نويسنده , , Lucille L’Heureux، نويسنده , , Richard Bethell، نويسنده , , et al.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
5333
To page
5337
Abstract
HCV NS5B RNA-dependent RNA polymerase (NS5B) is essential for viral replication and is therefore considered a target for antiviral drug development. From our ongoing screening effort in the search for new anti-HCV agents, a novel inhibitor 1 with low μM activity against the HCV NS5B polymerase was identified. SAR analysis indicated the optimal substitution pattern required for activity, for example, carboxylic acid group at 2-position of thiophene ring. We describe the steps taken to identify and solve the bioactive conformation of derivative 6 through the use of the transferred NOE method (trNOE).
Keywords
HCV , NS5B polymerase , Inhibitor.* Corresponding author. Tel.: +1 450 978 6435 , NMR , fax: +1 450 9787777 , e-mail: cyannopoulos@virochempharma.com
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794981
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