发现二苯甲烷类似物作为抗牛腹泻病毒剂
Discovery of diphenylmethane analogs as anti-bovine diarrhea viral agents.
作者信息
Hosoda Shinnosuke, Aoyama Hiroshi, Goto Yukinori, Salim Mohammed T A, Okamoto Mika, Hashimoto Mariko, Baba Masanori, Hashimoto Yuichi
机构信息
Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
出版信息
Bioorg Med Chem Lett. 2009 Jun 15;19(12):3157-61. doi: 10.1016/j.bmcl.2009.04.137. Epub 2009 May 3.
Based on antiviral screening of our diphenylmethane derivatives prepared as steroid substitutes, we identified a 1,1-diphenylcyclobutane analog (9) and two diethyldiphenylsilane analogs (12 and 13) as superior lead compounds with potent anti-bovine viral diarrhea virus (BVDV) activity, having 50% effective concentration (EC(50): based on reduction of BVDV replication-induced cell destruction) and 50% cytotoxic concentration (CC(50): based on reduction of viable cell number) values of 6.2-8.4 microM and >100 microM, respectively, in Madin-Darby bovine kidney (MDBK) cells infected with BVDV.
基于对我们制备的作为甾体替代物的二苯甲烷衍生物进行的抗病毒筛选，我们鉴定出一种1,1 - 二苯基环丁烷类似物（9）和两种二乙基二苯基硅烷类似物（12和13）作为具有强效抗牛病毒性腹泻病毒（BVDV）活性的优质先导化合物，在感染BVDV的马迪 - 达比牛肾（MDBK）细胞中，其50%有效浓度（EC50：基于BVDV复制诱导的细胞破坏的减少）和50%细胞毒性浓度（CC50：基于活细胞数量的减少）值分别为6.2 - 8.4微摩尔和>100微摩尔。
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