高效且具选择性的人类过氧化物酶体增殖物激活受体α激动剂的设计与合成
Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists.
作者信息
Yamazaki Yukiyoshi, Abe Kazutoyo, Toma Tsutomu, Nishikawa Masahiro, Ozawa Hidefumi, Okuda Ayumu, Araki Takaaki, Oda Soichi, Inoue Keisuke, Shibuya Kimiyuki, Staels Bart, Fruchart Jean-Charles
机构信息
Tokyo New Drug Research Laboratories 1, Pharmaceutical Division, Kowa Co., LTD, 2-17-43, Noguchicho, Higashimurayam, Tokyo 189-0022, Japan.
出版信息
Bioorg Med Chem Lett. 2007 Aug 15;17(16):4689-93. doi: 10.1016/j.bmcl.2007.05.066. Epub 2007 May 24.
A combination of benzoxazole, phenoxyalkyl side chain, and phenoxybutyric acids was identified as a highly potent and selective human peroxisome proliferator-activated receptor alpha (PPARalpha) agonist. The synthesis, structure-activity relationship (SAR) studies, and in vivo activities of the representative compounds are described.
苯并恶唑、苯氧基烷基侧链和苯氧基丁酸的组合被鉴定为一种高效且选择性的人类过氧化物酶体增殖物激活受体α（PPARα）激动剂。本文描述了代表性化合物的合成、构效关系（SAR）研究及体内活性。
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