de Clercq E
Antimicrob Agents Chemother. 1984 Aug;26(2):155-9. doi: 10.1128/AAC.26.2.155.
(E)-5-(2-Bromovinyl)-2'-deoxyuridine (bromovinyldeoxyuridine) was found to suppress the development of herpetic skin lesions and the paralysis and mortality associated therewith in hairless mice inoculated intracutaneously with herpes simplex virus type 1. This protective effect was achieved with bromovinyldeoxyuridine applied topically at 1, 3, or 10% in either dimethylsulfoxide (DMSO), Beeler base, Tween-glycerol-water, 5% Azone (1-dodecylazacycloheptan-2-one) in water, or 5% Azone in DMSO. The optimal vehicle was 5% Azone in DMSO, in which bromovinyldeoxyuridine was effective even at a concentration as low as 0.3%. In its protective activity against cutaneous herpes simplex virus type 1 infection in hairless mice, bromovinyldeoxyuridine was clearly superior to other established antiherpes compounds such as 5-iodo-2'-deoxyuridine, 5-ethyl-2'-deoxyuridine, arabinosyl thymine, and arabinosyl (E)-5-(2-bromovinyl) uracil when formulated at 10% in DMSO or Azone-DMSO. However, no activity was noted with any of these drug formulations against cutaneous herpes simplex virus type 2 infection. In contrast, acycloguanosine (acyclovir) proved quite effective in the topical treatment of cutaneous herpes simplex virus type 2 infection when used at 10% in DMSO or at 5% in propylene glycol.
发现（E）-5-（2-溴乙烯基）-2'-脱氧尿苷（溴乙烯基脱氧尿苷）可抑制单纯疱疹病毒1型皮内接种的无毛小鼠疱疹性皮肤损伤的发展以及与之相关的麻痹和死亡率。在二甲基亚砜（DMSO）、比勒尔基质、吐温-甘油-水、5%氮酮（1-十二烷基氮杂环庚烷-2-酮）水溶液或5%氮酮的DMSO溶液中，分别以1%、3%或10%的浓度局部应用溴乙烯基脱氧尿苷可实现这种保护作用。最佳载体是5%氮酮的DMSO溶液，其中溴乙烯基脱氧尿苷即使在低至0.3%的浓度下也有效。在对无毛小鼠皮肤单纯疱疹病毒1型感染的保护活性方面，当在DMSO或氮酮-DMSO中配制成10%时，溴乙烯基脱氧尿苷明显优于其他已确立的抗疱疹化合物，如5-碘-2'-脱氧尿苷、5-乙基-2'-脱氧尿苷、阿糖胸腺嘧啶和阿糖基（E）-5-（2-溴乙烯基）尿嘧啶。然而，这些药物制剂对皮肤单纯疱疹病毒2型感染均无活性。相比之下，阿昔洛韦在DMSO中以10%或在丙二醇中以5%使用时，在皮肤单纯疱疹病毒2型感染的局部治疗中证明相当有效。
