2. Academic Validation
  3. Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists

Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists

  • Bioorg Med Chem Lett. 2007 Jul 1;17(13):3595-8. doi: 10.1016/j.bmcl.2007.04.057.
Nam-Jung Kim 1,  Kwang-Ok Lee,  Bon-Woong Koo,  Funan Li,  Ja-Kyung Yoo,  Hyun-Ju Park,  Kyung-Hoon Min,  Joong In Lim,  Mi Kyung Kim,  Jin-Kwan Kim,  Young-Ger Suh
Affiliations

Affiliation

  • 1 College of Pharmacy, Seoul National University, Sillim-dong, Seoul, Republic of Korea.
PMID: 17507225 DOI: 10.1016/j.bmcl.2007.04.057
Abstract

We have developed a new class of PPARalpha/gamma dual agonists, which show excellent agonistic activity in PPARalpha/gamma transactivation assay. In particular, (R)-9d was identified as a potent PPARalpha/gamma dual agonist with EC(50)s of 0.377 microM in PPARalpha and 0.136 microM in PPARgamma, respectively. Interestingly, the structure-activity relationship revealed that the stereochemistry of the identified PPARalpha/gamma dual agonists significantly affects their agonistic activities in PPARalpha than in PPARgamma.

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