共查询到20条相似文献,搜索用时 15 毫秒
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Marilyn B. Kroeger Smith Stephen H. Hughes Paul L. Boyer Christopher J. Michejda Carol A. Rouzer Lisa A. Taneyhill Richard H. Smith Nathan A. Smith Paul A.J. Janssen Henri Moereels Luc Koymans Edward Arnold Jianping Ding Kalyan Das Wanyi Zhang 《Protein science : a publication of the Protein Society》1995,4(10):2203-2222
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Gomez R Jolly S Williams T Tucker T Tynebor R Vacca J McGaughey G Lai MT Felock P Munshi V DeStefano D Touch S Miller M Yan Y Sanchez R Liang Y Paton B Wan BL Anthony N 《Bioorganic & medicinal chemistry letters》2011,21(24):7344-7350
Next generation NNRTIs are sought which possess both broad spectrum antiviral activity against key mutant strains and a high genetic barrier to the selection of new mutant viral strains. Pyridones were evaluated as an acyclic conformational constraint to replace the aryl ether core of MK-4965 (1) and the more rigid indazole constraint of MK-6186 (2). The resulting pyridone compounds are potent inhibitors of HIV RT and have antiviral activity in cell culture that is superior to other next generation NNRTI’s. 相似文献
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《Bioorganic & medicinal chemistry》2014,22(4):1459-1467
A series of novel N1-aryl-2-arylthioacetamido-benzimidazoles were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Some of them proved to be effective in inhibiting HIV-1 replication at submicromolar and nanomolar concentration acting as HIV-1 non-nucleoside RT inhibitors (NNRTIs), with low cytotoxicity. The preliminary structure–activity relationship (SAR) of these new derivatives was discussed and rationalized by docking studies. 相似文献