| Structural highlights
Publication Abstract from PubMed
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.
Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.,Gomez R, Jolly S, Williams T, Tucker T, Tynebor R, Vacca J, McGaughey G, Lai MT, Felock P, Munshi V, DeStefano D, Touch S, Miller M, Yan Y, Sanchez R, Liang Y, Paton B, Wan BL, Anthony N Bioorg Med Chem Lett. 2011 Dec 15;21(24):7344-50. Epub 2011 Oct 17. PMID:22071300[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
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References
- ↑ Gomez R, Jolly S, Williams T, Tucker T, Tynebor R, Vacca J, McGaughey G, Lai MT, Felock P, Munshi V, DeStefano D, Touch S, Miller M, Yan Y, Sanchez R, Liang Y, Paton B, Wan BL, Anthony N. Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7344-50. Epub 2011 Oct 17. PMID:22071300 doi:10.1016/j.bmcl.2011.10.027
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