Novel 1,3-dicarbonyl compounds having 2(3H)-benzazolonic heterocycles as PPARgamma agonists.
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.
Blanc-Delmas
Elodie
E
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.
Lebegue
Nicolas
N
Wallez
Valérie
V
Leclerc
Véronique
V
Yous
Saïd
S
Carato
Pascal
P
Farce
Amaury
A
Bennejean
Caroline
C
Renard
Pierre
P
Caignard
Daniel-Henri
DH
Audinot-Bouchez
Valérie
V
Chomarat
Pascale
P
Boutin
Jean
J
Hennuyer
Nathalie
N
Louche
Katie
K
Carmona
Maria Carmen
MC
Staels
Bart
B
Pénicaud
Luc
L
Casteilla
Louis
L
Lonchampt
Michel
M
Dacquet
Catherine
C
Chavatte
Philippe
P
Berthelot
Pascal
P
Lesieur
Daniel
D
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
D001391:Azo Compounds; D006571:Heterocyclic Compounds; D047495:PPAR gamma