SYNTHESIS OF SOME PHOSPHONATES WITH ANTIHERPETIC ACTIVITY

被引:8
作者
DIANA, GD [1 ]
ZALAY, ES [1 ]
SALVADOR, UJ [1 ]
PANCIC, F [1 ]
STEINBERG, B [1 ]
机构
[1] STERLING WINTHROP RES INST, RENSSELAER, NY 12144 USA
关键词
D O I
10.1021/jm00371a024
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several keto phosphonates, phosphonoacetates and dialkyl phosphonates containing (aryloxy)aryl gorups were synthesized and evaluated for antiherpetic activity. Two of the most active compounds, 12 [ethyl 8-(2-chloro-4-methoxyphenoxy)-2-(diethoxyphosphinyl)octanoate] and 16 [diethyl [6-(2-chloro-4-methoxyphenoxy)hexyl]-phosphonate], 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.
引用
收藏
页码:691 / 694
页数:4
相关论文
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