Design and synthesis of 3, 4-dihydro-1H-[1]-benzothieno [2, 3-c] pyran and 3, 4-dihydro-1H-pyrano [3, 4-b] benzofuran derivatives as non-nucleoside inhibitors of HCV …

A Gopalsamy, A Aplasca, G Ciszewski, K Park…

Index: Gopalsamy, Ariamala; Aplasca, Alexis; Ciszewski, Gregory; Park, Kaapjoo; Ellingboe, John W.; Orlowski, Mark; Feld, Boris; Howe, Anita Y.M. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 2 p. 457 - 460

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Citation Number: 48

Abstract

A novel class of HCV NS5B RNA dependent RNA polymerase inhibitors containing 3, 4- dihydro-1H-[1]-benzothieno [2, 3-c] pyran and 3, 4-dihydro-1H-pyrano [3, 4-b] benzofuran scaffolds were designed and synthesized. Optimization of the alkyl substituent in the pyran ring showed preference for an n-propyl group, while 5, 8-disubstitution pattern is preferred for the aromatic region. Analog 19 displayed potent activity with an IC50 of 50nM against ...