Bioorganic & Medicinal Chemistry Letters ——个性化文献订阅—

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Non-nucleoside inhibitors of HCV polymerase NS5B. Part 2: Synthesis and structure-activity relationships of benzothiazine-substituted quinolinediones

作者	de Vicente, J; Hendricks, RT; Smith, DB; Fell, JB; Fischer, J; Spencer, SR; Stengel, PJ; Mohr, P; Robinson, JE; Blake, JF; Hilgenkamp, RK; Yee, C; Adjabeng, G; Elworthy, TR; Tracy, J; Chin, E; Li, J; Wang, B; Bamberg, JT; Stephenson, R; Oshiro, C; Harris, SF; Ghate, M; Leveque, V; Najera, I; Le Pogam, S; Rajyaguru, S; Ao-Ieong, G; Alexandrova, L; Larrabee, S; Brandl, M; Briggs, A; Sukhtankar, S; Farrell, R; Xu, B

选自	期刊 Bioorganic & Medicinal Chemistry Letters; 卷期 2009年19-13; 页码 3642-3646

关联知识点

[摘要]：A new series of benzothiazine-substituted quinolinediones were evaluated as inhibitors of HCV polymerase NS5B. SAR studies on this series revealed a methyl sulfonamide group as a high affinity feature. Analogues with this group showed submicromolar potencies in the HCV cell based replicon assay. Pharmacokinetic and toxicology studies were also performed on a selected compound (34) to evaluate in vivo properties of this new class of inhibitors of HCV NS5B polymerase. (C) 2009 Elsevier Ltd. All rights reserved.
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