Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase

…, T Tucker, R Tynebor, J Vacca, G McGaughey…

Index: Gomez, Robert; Jolly, Samson; Williams, Theresa; Tucker, Thomas; Tynebor, Robert; Vacca, Joe; McGaughey, Georgia; Lai, Ming-Tain; Felock, Peter; Munshi, Vandna; Destefano, Daniel; Touch, Sinoeun; Miller, Mike; Yan, Youwei; Sanchez, Rosa; Liang, Yuexia; Paton, Brenda; Wan, Bang-Lin; Anthony, Neville Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 24 p. 7344 - 7350

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Citation Number: 12

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 ...