title: Design and synthesis of benzoxazole containing indole analogs as peroxisome proliferator-activated receptor-γ/δ dual agonists.
abstract: A series of benzoxazole or benzothiazole containing indole analogs, 6-alkoxyindole-2-carboxylic acids and 5-alkoxy-3-indolylacetic acids, were synthesized as novel candidates of PPARγ/δ dual agonists and their ligand activities for PPAR subtypes (α, γ, and δ) were investigated. In transient transactivation assay, several compounds activated PPARγ and δ with little activity of PPARα. Putative binding mode of the compounds 1a and 2a in the active site of PPARγ was similar with that of rosiglitazone and the molecular modeling provides molecular insight to the observed activity.
authors.affiliation: College of Pharmacy, Sookmyung Women's University, 52 Hyochangwon-Gil, Yongsan-Ku, Seoul 140-742, South Korea.
authors.forename: Hyo Jin
authors.initials: HJ
authors.lastname: Gim
authors.forename: Ye-Jin
authors.initials: YJ
authors.lastname: Cheon
authors.forename: Jae-Ha
authors.initials: JH
authors.lastname: Ryu
authors.forename: Raok
authors.initials: R
authors.lastname: Jeon
mesh_terms: D000085:Acetates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D007211:Indoles / Q000737:chemistry*; D015394:Molecular Structure; D047495:PPAR gamma / Q000819:agonists*; D011485:Protein Binding / Q000187:drug effects
chemical_list: D000085:Acetates; D001583:Benzoxazoles; D002264:Carboxylic Acids; D007211:Indoles; D047495:PPAR gamma