Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376207 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
Abstract
Aryl-tetrahydropyridine derivatives were prepared and their PPARα/γ dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARα/γ dual agonist with an EC50 of 1.73 and 0.64 μM in hPPARα and γ, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.
Graphical abstractThe synthesis of the potent PPARα/γ dual agonist (S)-5b (EC50 = 1.73/0.64 μM (α/γ)) is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Eunkyung Kim, Chan Sun Park, Taedong Han, Myung-Ho Bae, Wonee Chong, Choong Hyun Lee, Young Ah Shin, Byung-Nak Ahn, Mi Kyung Kim, Chang Yell Shin, Moon Ho Son, Jin Kwan Kim, Ho Sang Moon, Hyun Joo Shim, Eun Jung Kim, Soon Hoe Kim, Joong In Lim,