Hall I H, Cocolas G H, Williams W L
J Pharm Sci. 1984 Dec;73(12):1819-20. doi: 10.1002/jps.2600731240.
A series of 4-pyrimidinecarboxylic acids were evaluated for hypolipidemic activity in mice at 20-30 mg/kg/d ip. A number of these derivatives were observed to be active at this dose. Substitution of the hydroxyl group in position 2 and 6 of the 4-pyrimidinecarboxylic acid with a sulfhydryl and an amino group, respectively, led to a compound which produced a greater than 40% reduction of serum cholesterol and triglyceride levels in mice. Similarly, a compound which was substituted with an amino group in position 2 and an isobutyl group in position 5 led to equally potent activity as a hypolipidemic agent.
对一系列4-嘧啶羧酸进行了评估,以研究其在小鼠体内以20-30mg/kg/d的剂量腹腔注射时的降血脂活性。观察到许多这些衍生物在此剂量下具有活性。分别用巯基和氨基取代4-嘧啶羧酸2位和6位的羟基,得到一种化合物,该化合物可使小鼠血清胆固醇和甘油三酯水平降低40%以上。同样,一种在2位被氨基取代且在5位被异丁基取代的化合物作为降血脂剂具有同样强的活性。