Synthesis and SAR optimization of diketo acid pharmacophore for HCV NS5B polymerase inhibition

…, A Basu, MR Patel, N Kaushik-Basu, TT Talele

文献索引：Bhatt, Aaditya; Gurukumar; Basu, Amartya; Patel, Maulik R.; Kaushik-Basu, Neerja; Talele, Tanaji T. European Journal of Medicinal Chemistry, 2011 , vol. 46, # 10 p. 5138 - 5145

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被引用次数: 7

摘要

Hepatitis C virus (HCV) NS5B polymerase is a key target for anti-HCV therapeutics development. Here we report the synthesis and biological evaluation of a new series of α, γ- diketo acids (DKAs) as NS5B polymerase inhibitors. We initiated structure–activity relationship (SAR) optimization around the furan moiety of compound 1a [IC50= 21.8 μM] to achieve more active NS5B inhibitors. This yielded compound 3a [IC50= 8.2 μM] bearing ...