| Literature DB >> 17658778 |
Hui Li1, Angelica Linton, John Tatlock, Javier Gonzalez, Allen Borchardt, Mel Abreo, Tanya Jewell, Leena Patel, Matthew Drowns, Sarah Ludlum, Mike Goble, Michele Yang, Julie Blazel, Ravi Rahavendran, Heather Skor, Stephanie Shi, Cristina Lewis, Shella Fuhrman.
Abstract
The discovery and optimization of a novel class of carbon-linked dihydropyrones as allosteric HCV NS5B polymerase inhibitors are presented. Replacement of the sulfur linker atom with carbon reduced compound acidity and greatly increased cell permeation. Further structure-activity relationship (SAR) studies led to the identification of compounds, exemplified by 23 and 24, with significantly improved antiviral activities in the cell-based replicon assay and favorable pharmacokinetic profiles.Entities:
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Year: 2007 PMID： 17658778 DOI： 10.1021/jm0704447
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446