Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists |
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| Authors: | Kim Eunkyung Park Chan Sun Han Taedong Bae Myung-Ho Chong Wonee Lee Choong Hyun Shin Young Ah Ahn Byung-Nak Kim Mi Kyung Shin Chang Yell Son Moon Ho Kim Jin Kwan Moon Ho Sang Shim Hyun Joo Kim Eun Jung Kim Soon Hoe Lim Joong In Lee Chun Ho |
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| Institution: | Yuhan Research Institute, Drug Discovery Laboratory, 416-1, Gongse-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-902, Republic of Korea. |
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| Abstract: | Aryl-tetrahydropyridine derivatives were prepared and their PPARalpha/gamma dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARalpha/gamma dual agonist with an EC(50) of 1.73 and 0.64 microM in hPPARalpha and gamma, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties. |
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