Biological activity of the hypolipidemic agent, N2-n-butylindazolone.
Biological activity of the hypolipidemic agent, N2-n-butylindazolone.
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DOI：
10.1002/jps.2600731232
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发表时间：
1984-12
影响因子：
3.8
通讯作者：
I. Hall;W. Williams;S. Wyrick;P. J. Voorstad
中科院分区：
文献类型：
--
作者：
I. Hall;W. Williams;S. Wyrick;P. J. Voorstad
以前，一系列的N-取代吲唑酮衍生物被证明是有效的降血脂剂在啮齿动物。最有效的药物N2-正丁基吲唑酮在20 mg/kg/d时可抑制胆固醇和脂肪酸合成所需的细胞质乙酰辅酶A水平以及sn-甘油-3-磷酸酰基转移酶和磷脂酸磷酸水解酶活性。肝脏、小肠和血清脂蛋白组分的脂质含量降低，而粪便排泄物中的脂质含量增加。口服给药后，肠道对胆固醇的吸收严重减少。N2-正丁基吲唑酮的作用模式似乎与具有降血脂活性的环状酰亚胺相似。
Previously, a series of N-substituted indazolone derivatives proved to be effective hypolipidemic agents in rodents. The most effective agent, N2-n-butylindazolone, at 20 mg/kg/d was shown to suppress the levels of cytoplasm acetyl coenzyme A required for cholesterol and fatty acid synthesis as well as sn-glycerol-3-phosphate acyl transferase and phosphatidate phosphohydrolase activities. Lipid content of the liver, small intestine, and serum lipoprotein fractions was lowered, whereas lipid content was increased in fecal excretions by drug treatment for 14 d. The absorption of orally administered cholesterol from the intestine was severely reduced after drug administration. The mode of action of N2-n-butylindazolone appears to be similar to cyclic imides possessing hypolipidemic activity.