(2R)-2-甲基色满-2-羧酸：作为降血脂药物的选择性过氧化物酶体增殖物激活受体α激动剂的发现
(2R)-2-methylchromane-2-carboxylic acids: discovery of selective PPARalpha agonists as hypolipidemic agents.
作者信息
Koyama Hiroo, Boueres Julia K, Miller Daniel J, Berger Joel P, MacNaul Karen L, Wang Pei-ran, Ippolito Marc C, Wright Samuel D, Agrawal Arun K, Moller David E, Sahoo Soumya P
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000 Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2005 Jul 15;15(14):3347-51. doi: 10.1016/j.bmcl.2005.05.028.
PMID:15950464
Abstract
A SAR study was conducted on chromane-2-carboxylic acid toward selective PPARalpha agonisim. As a result, highly potent, and selective PPARalpha agonists were discovered. The optimized compound 43 exhibited robust lowering of total cholesterol levels in hamster and dog animal models.
摘要
针对色满-2-羧酸进行了一项关于选择性PPARα激动作用的构效关系研究。结果发现了高效且选择性的PPARα激动剂。优化后的化合物43在仓鼠和犬动物模型中表现出显著降低总胆固醇水平的作用。
Zotero 插件