title: Design and synthesis of marine fungal phthalide derivatives as PPAR-γ agonists.
abstract: On the basis of a marine fungal phthalide (paecilocin A) skeleton, we synthesized 20 analogs and evaluated them for peroxisome proliferator-activated receptor gamma (PPAR-γ) binding and activation. Among these analogs, 6 and 7 had significant PPAR-γ binding activity, and 7 showed further PPAR-γ activation in rat liver Ac2F cells. In docking simulation, 7 formed H bonds with key amino acid residues of the PPAR-γ binding domain, and the overall positioning was similar to rosiglitazone. This new phthalide derivative is considered an interesting new molecular class of PPAR-γ ligands.
authors: College of Pharmacy, Pusan National University, Busan 609-735, Republic of Korea.
authors: Bin
authors: B
authors: Xiao
authors: Jun
authors: J
authors: Yin
authors: Minhi
authors: M
authors: Park
authors: Juan
authors: J
authors: Liu
authors: Jian Lin
authors: JL
authors: Li
authors: Eun La
authors: EL
authors: Kim
authors: Jongki
authors: J
authors: Hong
authors: Hae Young
authors: HY
authors: Chung
authors: Jee H
authors: JH
authors: Jung
mesh_terms: D000818:Animals; D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001667:Binding, Competitive; D002460:Cell Line; D015195:Drug Design; D008099:Liver / Q000737:chemistry; D008958:Models, Molecular; D015394:Molecular Structure; D047495:PPAR gamma / Q000819:agonists*; D051381:Rats
chemical_list: D001572:Benzofurans; D047495:PPAR gamma; C082022:phthalide