Novel Hepatitis C virus replicon inhibitors: Synthesis and structure–activity relationships of fused pyrimidine derivatives

…, DW Beno, DA Betebenner, R Carrick, BE Green…

Index: Chris Krueger; Madigan, Darold L.; Beno, David W.; Betebenner, David A.; Carrick, Robert; Green, Brian E.; He, Wenping; Liu, Dachun; Maring, Clarence J.; McDaniel, Keith F.; Mo, Hongmei; Molla, Akhteruzzaman; Motter, Christopher E.; Pilot-Matias, Tami J.; Tufano, Michael D.; Kempf, Dale J. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2212 - 2215

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Citation Number: 15

Abstract

Our research team has been pursuing inhibition of the Hepatitis C virus by targeting several non-structural viral enzymes. 5 We have also initiated a broad screening program towards identifying novel leads that have antiviral potency in a HCV subgenomic replicon assay. 6 One such lead was a substituted naphthyridine derivative (1), shown in Table 1. We were pleased with the genotype 1b replicon potency of (EC 50 18 nM) as a starting point and hoped to improve upon the ...