title: Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
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.
authors.affiliation: Yuhan Research Institute, Drug Discovery Laboratory, 416-1, Gongse-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-902, Republic of Korea.
authors.forename: Eunkyung
authors.initials: E
authors.lastname: Kim
authors.forename: Chan Sun
authors.initials: CS
authors.lastname: Park
authors.forename: Taedong
authors.initials: T
authors.lastname: Han
authors.forename: Myung-Ho
authors.initials: MH
authors.lastname: Bae
authors.forename: Wonee
authors.initials: W
authors.lastname: Chong
authors.forename: Choong Hyun
authors.initials: CH
authors.lastname: Lee
authors.forename: Young Ah
authors.initials: YA
authors.lastname: Shin
authors.forename: Byung-Nak
authors.initials: BN
authors.lastname: Ahn
authors.forename: Mi Kyung
authors.initials: MK
authors.lastname: Kim
authors.forename: Chang Yell
authors.initials: CY
authors.lastname: Shin
authors.forename: Moon Ho
authors.initials: MH
authors.lastname: Son
authors.forename: Jin Kwan
authors.initials: JK
authors.lastname: Kim
authors.forename: Ho Sang
authors.initials: HS
authors.lastname: Moon
authors.forename: Hyun Joo
authors.initials: HJ
authors.lastname: Shim
authors.forename: Eun Jung
authors.initials: EJ
authors.lastname: Kim
authors.forename: Soon Hoe
authors.initials: SH
authors.lastname: Kim
authors.forename: Joong In
authors.initials: JI
authors.lastname: Lim
authors.forename: Chun Ho
authors.initials: CH
authors.lastname: Lee
mesh_terms: D000818:Animals; D020650:Combinatorial Chemistry Techniques; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D004195:Disease Models, Animal; D015195:Drug Design; D051379:Mice; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D047493:PPAR alpha; D047495:PPAR gamma; D011725:Pyridines