Shigeta S, Yokota T, Iwabuchi T, Baba M, Konno K, Ogata M, De Clercq E
J Infect Dis. 1983 Mar;147(3):576-84. doi: 10.1093/infdis/147.3.576.
Twenty antiherpes compounds were compared for their inhibitory activities against five laboratory strains and five clinical isolates of varicella-zoster virus (VZV) in human embryo fibroblast cultures. E-5-(2-bromovinyl)-1-beta-D-arabinofuranosyluracil (BVaraU), E-5-(2-iodovinyl)-2'-deoxyuridine (IVDU), and E-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) were the most effective. The average values of the 50% inhibitory dose (ID50) for VZV replication were 0.0013, 0.0015, and 0.0024 micrograms/ml, respectively. 1-beta-D-Arabinofuranosyladenine and 9-(2-hydroxyethoxymethyl)guanine were 1.2 and 3.4 times less effective than 5-iodo-2'-deoxyuridine (IDU). The selectivity indexes (ratio of ID50 for host-cell DNA synthesis to ID50 for VZV replication) of BVaraU, IVDU, and BVDU were between 41,000 and 67,000, whereas those of cytosine arabinoside, IDU, and 5-bromo-2'-deoxyuridine were less than 1.1. BVaraU, IVDU, and BVDU were the most potent and the most selective inhibitors of VZV activity. A deoxythymidine kinase deficient mutant of VZV was resistant to most of the compounds tested at concentrations up to 36,000 times greater than the average ID50 for strains that were not deficient.
在人胚成纤维细胞培养物中，比较了20种抗疱疹化合物对水痘 - 带状疱疹病毒（VZV）的5个实验室菌株和5个临床分离株的抑制活性。E - 5 -（2 - 溴乙烯基）-1 - β - D - 阿拉伯呋喃糖基尿嘧啶（BVaraU）、E - 5 -（2 - 碘乙烯基）-2'-脱氧尿苷（IVDU）和E - 5 -（2 - 溴乙烯基）-2'-脱氧尿苷（BVDU）最为有效。VZV复制的50%抑制剂量（ID50）的平均值分别为0.0013、0.0015和0.0024微克/毫升。1 - β - D - 阿拉伯呋喃糖基腺嘌呤和9 -（2 - 羟基乙氧基甲基）鸟嘌呤的效力分别比5 - 碘 - 2'-脱氧尿苷（IDU）低1.2倍和3.4倍。BVaraU、IVDU和BVDU的选择性指数（宿主细胞DNA合成的ID50与VZV复制的ID50之比）在41,000至67,000之间，而阿糖胞苷、IDU和5 - 溴 - 2'-脱氧尿苷的选择性指数小于1.1。BVaraU、IVDU和BVDU是VZV活性最有效和最具选择性的抑制剂。VZV的一种脱氧胸苷激酶缺陷型突变体对所测试的大多数化合物具有抗性，其浓度比非缺陷菌株的平均ID50高36,000倍。
