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Bioorg Med Chem Lett. 2009 Aug 1;19(15):4350-3. doi: 10.1016/j.bmcl.2009.05.091. Epub 2009 May 28.

Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase.

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  • 1Department of Medicinal Chemistry, GlaxoSmithKline, Collegeville, PA 19426, USA.


The synthesis and optimisation of HCV NS5B polymerase inhibitors with improved potency versus the existing compound 1 is described. Substitution in the benzothiadiazine portion of the molecule, furnishing improvement in potency in the high protein Replicon assay, is highlighted, culminating in the discovery of 12h, a highly potent oxyacetamide derivative.

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