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ID: ALA1137155

Journal: Bioorg Med Chem Lett

Title: Identification of [(naphthalene-1-carbonyl)-amino]-acetic acid derivatives as nonnucleoside inhibitors of HCV NS5B RNA dependent RNA polymerase.

Authors: Gopalsamy A, Lim K, Ellingboe JW, Krishnamurthy G, Orlowski M, Feld B, van Zeijl M, Howe AY.

Abstract: A novel series of HCV NS5B RNA dependent RNA polymerase inhibitors containing a naphthalene carboxamide scaffold were identified by high throughput screening. Optimization of substituents by parallel synthesis and the iterative design towards understanding structure-activity relationship to improve potency are described. Tetra substituted naphthalene 31 displayed potent activity with IC(50) of 120 nM against HCV NS5B enzyme and was selective over a panel of polymerases.

CiteXplore: 15261274

DOI: 10.1016/j.bmcl.2004.06.013