title: Novel 1,3-dicarbonyl compounds having 2(3H)-benzazolonic heterocycles as PPARgamma agonists.
abstract: A series of 1,3-dicarbonyl compounds having 2(3H)-benzazolonic heterocycles has been synthesized and tested for PPARgamma agonist activity. SAR were developed and revealed that 6-acyl-2(3H)-benzothiazolone derivatives with 1,3-dicarbonyl group were the most potent. IP administration of compound 22 exhibited comparable levels of glucose and triglyceride correction to PO administration of rosiglitazone in the ob/ob mouse studies.
authors.affiliation: Laboratoire de Chimie Thérapeutique EA1043, Faculté des Sciences Pharmaceutiques et Biologiques de Lille, 3 rue du Professeur Laguesse, B.P. 83 59006 LILLE Cedex, France.
authors.forename: Elodie
authors.initials: E
authors.lastname: Blanc-Delmas
authors.forename: Nicolas
authors.initials: N
authors.lastname: Lebegue
authors.forename: Valérie
authors.initials: V
authors.lastname: Wallez
authors.forename: Véronique
authors.initials: V
authors.lastname: Leclerc
authors.forename: Saïd
authors.initials: S
authors.lastname: Yous
authors.forename: Pascal
authors.initials: P
authors.lastname: Carato
authors.forename: Amaury
authors.initials: A
authors.lastname: Farce
authors.forename: Caroline
authors.initials: C
authors.lastname: Bennejean
authors.forename: Pierre
authors.initials: P
authors.lastname: Renard
authors.forename: Daniel-Henri
authors.initials: DH
authors.lastname: Caignard
authors.forename: Valérie
authors.initials: V
authors.lastname: Audinot-Bouchez
authors.forename: Pascale
authors.initials: P
authors.lastname: Chomarat
authors.forename: Jean
authors.initials: J
authors.lastname: Boutin
authors.forename: Nathalie
authors.initials: N
authors.lastname: Hennuyer
authors.forename: Katie
authors.initials: K
authors.lastname: Louche
authors.forename: Maria Carmen
authors.initials: MC
authors.lastname: Carmona
authors.forename: Bart
authors.initials: B
authors.lastname: Staels
authors.forename: Luc
authors.initials: L
authors.lastname: Pénicaud
authors.forename: Louis
authors.initials: L
authors.lastname: Casteilla
authors.forename: Michel
authors.initials: M
authors.lastname: Lonchampt
authors.forename: Catherine
authors.initials: C
authors.lastname: Dacquet
authors.forename: Philippe
authors.initials: P
authors.lastname: Chavatte
authors.forename: Pascal
authors.initials: P
authors.lastname: Berthelot
authors.forename: Daniel
authors.initials: D
authors.lastname: Lesieur
mesh_terms: D000818:Animals; D001391:Azo Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D002460:Cell Line; D015195:Drug Design; D005260:Female; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008958:Models, Molecular; D015394:Molecular Structure; D047495:PPAR gamma / Q000819:agonists* / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001391:Azo Compounds; D006571:Heterocyclic Compounds; D047495:PPAR gamma