Töpke H, Gräf M, Wutzler P, Herrmann G, Reefschläger J
Clinic of Eye Diseases, Medical Academy Erfurt, D.D.R.
Antiviral Res. 1988 Jul;9(4):273-80. doi: 10.1016/0166-3542(88)90058-7.
The 5-substituted 1-beta-D-arabinofuranosyl (araU) analogues, (E)-5-(2-bromovinyl)-araU (BrVaraU) and 5-vinyl-araU (VaraU), which can be considered as structural analogues of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BrVUdR), are potent and selective inhibitors of herpes simplex virus type 1 (HSV-1) replication in vitro. BrVaraU and VaraU have been compared with BrVUdR for their therapeutic effect on acute HSV-1 keratitis in rabbits. Both araU derivatives applied as 0.1% eyedrops suppressed the development of keratitis as monitored by the reduced number of herpes efflorescences. The healing effect of BrVaraU and VaraU was less pronounced than that of 0.1% BrVUdR eyedrops, the difference between BrVUdR and VaraU being statistically significant at the 10th day of treatment. As a further indication of the healing effect the number of cornea with opacities seen after cessation of drug treatment were 3.3, 7.4, 27.6 and 46.9% for the BrVUdR-BrVaraU-, VaraU- and placebo-treated eyes, respectively.
5-取代的1-β-D-阿拉伯呋喃糖基（araU）类似物，（E）-5-（2-溴乙烯基）-araU（BrVaraU）和5-乙烯基-araU（VaraU），可被视为（E）-5-（2-溴乙烯基）-2'-脱氧尿苷（BrVUdR）的结构类似物，是体外单纯疱疹病毒1型（HSV-1）复制的强效和选择性抑制剂。已将BrVaraU和VaraU与BrVUdR对兔急性HSV-1角膜炎的治疗效果进行了比较。两种araU衍生物以0.1%眼药水给药时，通过减少疱疹疹的数量监测，均抑制了角膜炎的发展。BrVaraU和VaraU的愈合效果不如0.1% BrVUdR眼药水明显，在治疗第10天时，BrVUdR和VaraU之间的差异具有统计学意义。作为愈合效果的进一步指标，停药后出现混浊的角膜数量在BrVUdR、BrVaraU、VaraU和安慰剂治疗组眼中分别为3.3%、7.4%、27.6%和46.9%。
