Title of article
Design, synthesis, and structure–activity relationship of carbamate-tethered aryl propanoic acids as novel PPARα/γ dual agonists
Author/Authors
Nam-Jung Kim، نويسنده , , Kwang-Ok Lee، نويسنده , , Bon-Woong Koo، نويسنده , , Funan Li، نويسنده , , Ja-Kyung Yoo، نويسنده , , Hyun Ju Park، نويسنده , , Kyung-Hoon Min، نويسنده , , Joong-Yeon Lim، نويسنده , , Mi Kyung Kim، نويسنده , , Jin-Kwan Kim، نويسنده , , Young-Ger Suh، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
3595
To page
3598
Abstract
We have developed a new class of PPARα/γ dual agonists, which show excellent agonistic activity in PPARα/γ transactivation assay. In particular, (R)-9d was identified as a potent PPARα/γ dual agonist with EC50s of 0.377 μM in PPARα and 0.136 μM in PPARγ, respectively. Interestingly, the structure–activity relationship revealed that the stereochemistry of the identified PPARα/γ dual agonists significantly affects their agonistic activities in PPARα than in PPARγ.
Keywords
Type 2 diabetes , PPARs , PPAR?/? dual agonists
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798277
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