Document Report Card

Basic Information

ID: ALA1148590

Journal: Bioorg Med Chem Lett

Title: 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 NS5B RNA dependent RNA polymerase.

Authors: Gopalsamy A, Aplasca A, Ciszewski G, Park K, Ellingboe JW, Orlowski M, Feld B, Howe AY.

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 IC(50) of 50 nM against HCV NS5B enzyme and was selective over a panel of polymerases.

CiteXplore: 16274990

DOI: 10.1016/j.bmcl.2005.08.114