Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370145 | Bioorganic & Medicinal Chemistry Letters | 2011 | 7 Pages |
Abstract
Next generation NNRTIs are sought which possess both broad spectrum antiviral activity against key mutant strains and a high genetic barrier to the selection of new mutant viral strains. Pyridones were evaluated as an acyclic conformational constraint to replace the aryl ether core of MK-4965 (1) and the more rigid indazole constraint of MK-6186 (2). The resulting pyridone compounds are potent inhibitors of HIV RT and have antiviral activity in cell culture that is superior to other next generation NNRTI’s.
Graphical abstractPyridone inhibitors of non-nucleoside reverse transcriptase (NNRTI) with improved potency are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Robert Gomez, Samson Jolly, Theresa Williams, Thomas Tucker, Robert Tynebor, Joe Vacca, Georgia McGaughey, Ming-Tain Lai, Peter Felock, Vandna Munshi, Daniel DeStefano, Sinoeun Touch, Mike Miller, Youwei Yan, Rosa Sanchez, Yuexia Liang, Brenda Paton,