Dygos J H, Jett C M, Chinn L J, Miller J E
J Med Chem. 1977 Dec;20(12):1705-8. doi: 10.1021/jm00222a039.
Several 5-aryl-3-methylvaleric acid derivatives have been shown to be more potent hypolipidemic agents than the previously reported 5-(4-biphenylyl)-3-methylvaleric acid (1). The most active compound in this series was 5-(4-phenylsulfonylphenyl)-3-methylvaleric acid (10) which lowered serum cholesterol levels 45% and serum triglyceride levels 60% in normal rats. Significant lowering of the serum triglyceride levels was the predominant effect noted with most of the compounds tested.
几种5-芳基-3-甲基戊酸衍生物已被证明是比先前报道的5-(4-联苯基)-3-甲基戊酸(1)更有效的降血脂剂。该系列中最具活性的化合物是5-(4-苯基磺酰基苯基)-3-甲基戊酸(10),它使正常大鼠的血清胆固醇水平降低了45%,血清甘油三酯水平降低了60%。在所测试的大多数化合物中,血清甘油三酯水平的显著降低是主要的作用。