Aryl uracil inhibitors of hepatitis C virus NS5B polymerase: Synthesis and characterization of analogs with a fused 5, 6-bicyclic ring motif

…, PL Donner, CA Flentge, DK Hutchinson, D Liu…

Index: Krueger, A. Chris; Randolph, John T.; Degoey, David A.; Donner, Pamela L.; Flentge, Charles A.; Hutchinson, Douglas K.; Liu, Dachun; Motter, Christopher E.; Rockway, Todd W.; Wagner, Rolf; Beno, David W.A.; Koev, Gennadiy; Lim, Hock B.; Beyer, Jill M.; Mondal, Rubina; Liu, Yaya; Kati, Warren M.; Longenecker, Kenton L.; Molla, Akhteruzzaman; Stewart, Kent D.; Maring, Clarence J. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 12 p. 3487 - 3490

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Abstract

The synthesis and structure–activity relationships of a novel aryl uracil series which contains a fused 5, 6-bicyclic ring unit for HCV NS5B inhibition is described. Several analogs display replicon cell culture potencies in the low nanomolar range along with excellent rat pharmacokinetic values.

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