Inhibitors of HCV NS5B polymerase: Synthesis and structure–activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1, 8-naphthyridon-3-yl …

…, KF McDaniel, JK Pratt, D Beno, D Montgomery…

Index: Rockway, Todd W.; Zhang, Rong; Liu, Dachun; Betebenner, David A.; McDaniel, Keith F.; Pratt, John K.; Beno, David; Montgomery, Debra; Jiang, Wen W.; Masse, Sherie; Kati, Warren M.; Middleton, Tim; Molla, Akhteruzzaman; Maring, Clarence J.; Kempf, Dale J. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 14 p. 3833 - 3838

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Citation Number: 35

Abstract

A series of non-nucleoside HCV NS5B polymerase inhibitors based on the N-1-benzyl or N- 1-[3-methylbutyl]-4-hydroxy-1, 8-naphthyridon-3-yl benzothiadiazine core substituted in the D-ring aromatic moiety have been prepared and evaluated. Aromatic substituents extending from position 7 of the D-ring exhibited excellent potency against both genotypes 1a and 1b.