Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists |
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Authors: | Kim Nam-Jung Lee Kwang-Ok Koo Bon-Woong Li Funan Yoo Ja-Kyung Park Hyun-Ju Min Kyung-Hoon Lim Joong In Kim Mi Kyung Kim Jin-Kwan Suh Young-Ger |
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Institution: | College of Pharmacy, Seoul National University, Sillim-dong, Seoul, Republic of Korea. |
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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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