Autor: |
John O'Connell, Kevin J. Curran, Kristine Svenson, Anita Y. M. Howe, Kitae Lim, Steven F. Sukits, Mengxiao Shi, Ariamala Gopalsamy, Boris Feld, Girija Krishnamurthy, Rajiv Chopra, Tarek S. Mansour, Atul Agarwal, Mark Orlowski, Joel Bard, John W. Ellingboe, Gregory Ciszewski |
Rok vydání: |
2006 |
Předmět: |
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Zdroj: |
Journal of Medicinal Chemistry. 49:3052-3055 |
ISSN: |
1520-4804 0022-2623 |
Popis: |
Through high throughput screening, substituted proline sulfonamide 6 was identified as HCV NS5b RNA-dependent RNA polymerase inhibitor. Optimization of various regions of the lead molecule resulted in compounds that displayed good potency and selectivity. The crystal structure of 6 and NS5b polymerase complex confirmed the binding near the active site region. The optimization approach and SAR are discussed in detail. |
Databáze: |
OpenAIRE |
Externí odkaz: |
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