Tompkins J E
J Med Chem. 1986 May;29(5):855-9. doi: 10.1021/jm00155a042.
A series of 5,5-diaryl-2-thiohydantoins and 5,5-diaryl-N3-substituted-2-thiohydantoins related to 5,5-diphenyl-2-thiohydantoin (DPTH) were investigated as potential hypolipidemic agents with the goal of increased potency over DPTH itself. In the 5,5-diaryl class, the best results were obtained by substituting two pyridyl rings for the phenyl rings found in DPTH. The resulting compound, 5,5-bis(2-pyridyl)-2-thiohydantoin, DPYTH (5), had slightly better activity than DPTH in lowering liver cholesterol values. Further modifications to DPYTH (5) are underway and will be the subject of a future report. In the N3 nitrogen-substituted series one compound, 5,5-diphenyl-N3-n-butyl-2-thiohydantoin, DPBTH (7), showed promise during initial screening, but when analyzed in a dose-response study, its activity was considerably less than that of the parent compound DPTH.
研究了一系列与5,5-二苯基-2-硫代乙内酰脲（DPTH）相关的5,5-二芳基-2-硫代乙内酰脲和5,5-二芳基-N3-取代-2-硫代乙内酰脲，作为潜在的降血脂药物，目标是比DPTH本身具有更高的效力。在5,5-二芳基类别中，用两个吡啶环取代DPTH中的苯环得到了最佳结果。所得化合物5,5-双（2-吡啶基）-2-硫代乙内酰脲，即DPYTH（5），在降低肝脏胆固醇值方面的活性略优于DPTH。对DPYTH（5）的进一步修饰正在进行中，将是未来一篇报告的主题。在N3氮取代系列中，一种化合物5,5-二苯基-N3-正丁基-2-硫代乙内酰脲，即DPBTH（7），在初步筛选中显示出前景，但在剂量反应研究中分析时，其活性远低于母体化合物DPTH。
