Reefschläger J, Wutzler P, Thiel K D, Herrmann G
Antiviral Res. 1986 Mar;6(2):83-93. doi: 10.1016/0166-3542(86)90028-8.
The efficiency of (E)-5-(2-bromovinyl)- and 5-vinyl-1-beta-D-arabinofuranosyluracil (BrVaraU, VaraU) as inhibitors of three herpes simplex virus type 1 (HSV-1) strains was assessed in comparison to (E)-5-(2-bromovinyl)-2'-deoxyuridine (BrVUdR), 9-(2-hydroxyethoxymethyl)guanine (ACV), and trisodium phosphonoformate (Na3PFA) using a plaque assay in human embryonic lung fibroblast (HELF) cell cultures. The following order of decreasing activity was found: BrVaraU greater than VaraU greater than BrVU-dR greater than ACV much greater than Na3PFA. In HELF cell cultures, the selectivity indexes of VaraU and BrVaraU were 10 times higher than those of BrVUdR and ACV. Protection of mice from encephalitis and death due to intracerebral (i.c.) infection with a clinical HSV-1 isolate was nearly complete if mice were treated intraperitoneally (i.p.) with two daily doses of VaraU and BrVaraU (100 or 200 mg/kg per day) over a period of 5 or 10 days. The efficacy was similar to ACV, but, using a treatment schedule of three daily i.p. doses over 10 days, with equimolar amounts of the nucleoside analogs, VaraU and BrVaraU (140 and 180 mg/kg per day) were superior to ACV (130 mg/kg per day) (P less than 0.05).
在人胚肺成纤维细胞（HELF）培养物中，采用蚀斑试验，将（E）-5-（2-溴乙烯基）-和5-乙烯基-1-β-D-阿拉伯呋喃糖基尿嘧啶（BrVaraU、VaraU）作为三种单纯疱疹病毒1型（HSV-1）毒株抑制剂的效率，与（E）-5-（2-溴乙烯基）-2'-脱氧尿苷（BrVUdR）、9-（2-羟乙氧甲基）鸟嘌呤（阿昔洛韦）和膦甲酸钠（Na3PFA）进行了比较。发现活性由高到低的顺序如下：BrVaraU＞VaraU＞BrVU-dR＞阿昔洛韦＞＞Na3PFA。在HELF细胞培养物中，VaraU和BrVaraU的选择性指数比BrVUdR和阿昔洛韦高10倍。如果小鼠在5天或10天内每天腹腔注射（i.p.）两次VaraU和BrVaraU（每天100或200mg/kg），则对临床HSV-1分离株脑内（i.c.）感染所致脑炎和死亡的保护作用几乎是完全的。其疗效与阿昔洛韦相似，但采用在10天内每天腹腔注射三次的治疗方案，使用等摩尔量的核苷类似物VaraU和BrVaraU（每天140和180mg/kg）优于阿昔洛韦（每天130mg/kg）（P＜0.05）。
