Identification of novel PPARα ligands by the structural modification of a PPARγ ligand

Identification of novel PPARα ligands by the structural modification of a PPARγ ligand
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通过 PPARγ 配体的结构修饰鉴定新型 PPARα 配体

DOI:
10.1016/j.bmcl.2006.03.031
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发表时间:
2006
影响因子:
2.7
通讯作者:
N. Miyata
N. Miyata
中科院分区:
医学4区
文献类型:
--
作者:
Shinya Usui;Hiroki Fujieda;Takayoshi Suzuki;Naoaki Yoshida;H. Nakagawa;N. Miyata

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为了开发新型 PPARα 配体,我们设计并合成了几种 3-{3-[2-(壬基吡啶-2-基氨基)乙氧基]苯基}丙酸衍生物。化合物 10 是 PPARγ 激动剂 1 的间位异构体,已被鉴定为 PPARα 配体。在10的丙酸的C-2位置引入甲基和乙基进一步提高了PPARα结合效力。
To develop novel PPARα ligands, we designed and synthesized several 3-{3-[2-(nonylpyridin-2-ylamino)ethoxy]phenyl}propanoic acid derivatives. Compound 10, the meta isomer of a PPARγ agonist 1, has been identified as a PPARα ligand. The introduction of methyl and ethyl groups at the C-2 position of the propanoic acid of 10 further improved the PPARα-binding potency.
DOI: 10.1016/j.bmcl.2005.10.049
发表时间: 2006-02
影响因子: 2.7
作者:
Jun-ichi Kasuga;M. Makishima;Y. Hashimoto;H. Miyachi
通讯作者: Jun-ichi Kasuga;M. Makishima;Y. Hashimoto;H. Miyachi
DOI: 10.1016/j.bmcl.2005.01.074
发表时间: 2005-03
影响因子: 2.7
作者:
Shinya Usui;Takayoshi Suzuki;Y. Hattori;Kazuma Etoh;Hiroki Fujieda;M. Nishizuka;M. Imagawa;H. Nakagawa
通讯作者: Shinya Usui;Takayoshi Suzuki;Y. Hattori;Kazuma Etoh;Hiroki Fujieda;M. Nishizuka;M. Imagawa;H. Nakagawa