一些具有抗疱疹活性的膦酸酯的合成。

Synthesis of some phosphonates with antiherpetic activity.

作者信息

Diana G D, Zalay E S, Salvador U J, Pancic F, Steinberg B

出版信息

J Med Chem. 1984 May;27(5):691-4. doi: 10.1021/jm00371a024.

Abstract

Several keto phosphonates, phosphonoacetates , and dialkyl phosphonates containing (aryloxy)aryl groups were synthesized and evaluated for antiherpteic activity. Two of the most active compounds, 12 and 16, were evaluated topically in the mouse vaginal model against herpes simplex virus (HSV) type 2. Compound 16 exhibited an increased survival rate, as well as increased survival time. Evaluation of 16 in the guinea pig skin test against HSV-2 produced a reduction in virus titer, as well as in mean vesicle score.

摘要

合成了几种含有（芳氧基）芳基的酮膦酸酯、膦酰基乙酸酯和二烷基膦酸酯，并对其抗疱疹活性进行了评估。对两种活性最高的化合物12和16在小鼠阴道模型中进行了针对2型单纯疱疹病毒（HSV）的局部评估。化合物16显示出存活率提高以及存活时间延长。在豚鼠皮肤试验中对16针对HSV - 2的评估显示病毒滴度以及平均水疱评分降低。