Novel 1,3-dicarbonyl compounds having 2(3H)-benzazolonic heterocycles as PPARγ agonists
2006; Elsevier BV; Volume: 14; Issue: 22 Linguagem: Inglês
10.1016/j.bmc.2006.07.029
ISSN1464-3391
AutoresElodie Blanc-Delmas, Nicolas Lebègue, Valérie Wallez, Véronique Leclerc, Saı̈d Yous, Pascal Carato, Amaury Farce, Caroline Bennejean, Pierre Renard, Daniel‐Henri Caignard, Valérie Audinot‐Bouchez, Pascale Chomarat, Jean A. Boutin, Nathalie Hennuyer, Katie Louche, Maria Carmen Carmona, Bart Staels, Luc Pénicaud, Louis Casteilla, Michel Lonchampt, Catherine Dacquet, Philippe Chavatte, Pascal Berthelot, Daniel Lesieur,
Tópico(s)NF-κB Signaling Pathways
ResumoA 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.
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