Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase
| Autor: | Yuexia Liang, Daniel DeStefano, Samson M. Jolly, Georgia B. McGaughey, Joe P. Vacca, Bang-Lin Wan, Michael W. Miller, Robert P. Gomez, Youwei Yan, Sinoeun Touch, Neville J. Anthony, Robert M. Tynebor, Ming-Tain Lai, Rosa I. Sanchez, Vandna Munshi, Thomas J. Tucker, Theresa M. Williams, Peter J. Felock, Brenda Paton |
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| Rok vydání: | 2011 |
| Předmět: |
Pyridines
Pyridones Stereochemistry Clinical Biochemistry Mutant Pharmaceutical Science Ether Biochemistry Cell Line chemistry.chemical_compound Protein structure Drug Discovery Humans Computer Simulation Binding site Molecular Biology Indazole Binding Sites Organic Chemistry HIV virus diseases HIV Reverse Transcriptase Reverse transcriptase Protein Structure Tertiary Enzyme Activation chemistry Cell culture Drug Design Pyrazoles Reverse Transcriptase Inhibitors Molecular Medicine Nucleoside |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 21:7344-7350 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2011.10.027 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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