title: Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
abstract: Oxime ethers of alpha-acyl-beta-phenylpropanoic acids were prepared to apply as PPARalpha and gamma dual agonists. Among them, compound 11l proved to exhibit potent in vitro activities with EC(50) of 19 and 13nM in PPARalpha and gamma, respectively. It showed better glucose lowering effects than rosiglitazone 1 and ameliorated the lipid profile like plasma triglyceride in db/db mice model.
authors.affiliation: Research and Development, LG Life Sciences, 104-1 Munji-dong, Yuseong-gu, Daejon 305-380, Republic of Korea.
authors.forename: Hee
authors.initials: H
authors.lastname: Oon Han
authors.forename: Seung Hae
authors.initials: SH
authors.lastname: Kim
authors.forename: Kyoung-Hee
authors.initials: KH
authors.lastname: Kim
authors.forename: Gwong-Cheung
authors.initials: GC
authors.lastname: Hur
authors.forename: Hyeon
authors.initials: H
authors.lastname: Joo Yim
authors.forename: Hee-Kyung
authors.initials: HK
authors.lastname: Chung
authors.forename: Sung
authors.initials: S
authors.lastname: Ho Woo
authors.forename: Ki
authors.initials: K
authors.lastname: Dong Koo
authors.forename: Chang-Seok
authors.initials: CS
authors.lastname: Lee
authors.forename: Jong
authors.initials: J
authors.lastname: Sung Koh
authors.forename: Geun Tae
authors.initials: GT
authors.lastname: Kim
mesh_terms: D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D001786:Blood Glucose / Q000378:metabolism; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D007202:Indicators and Reagents; D008055:Lipids / Q000097:blood; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D008958:Models, Molecular; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000494:pharmacology*; D000077154:Rosiglitazone; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000494:pharmacology; D014280:Triglycerides / Q000097:blood
chemical_list: D001786:Blood Glucose; D007004:Hypoglycemic Agents; D007202:Indicators and Reagents; D008055:Lipids; D047493:PPAR alpha; D047495:PPAR gamma; D010666:Phenylpropionates; D045162:Thiazolidinediones; D014280:Triglycerides; D000077154:Rosiglitazone