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  • Title: Identification of [(naphthalene-1-carbonyl)-amino]-acetic acid derivatives as nonnucleoside inhibitors of HCV NS5B RNA dependent RNA polymerase.
    Author: Gopalsamy A, Lim K, Ellingboe JW, Krishnamurthy G, Orlowski M, Feld B, van Zeijl M, Howe AY.
    Journal: Bioorg Med Chem Lett; 2004 Aug 16; 14(16):4221-4. PubMed ID: 15261274.
    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.
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