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  • Title: Novel 1,3-dicarbonyl compounds having 2(3H)-benzazolonic heterocycles as PPARgamma agonists.
    Author: Blanc-Delmas E, Lebegue N, Wallez V, Leclerc V, Yous S, Carato P, Farce A, Bennejean C, Renard P, Caignard DH, Audinot-Bouchez V, Chomarat P, Boutin J, Hennuyer N, Louche K, Carmona MC, Staels B, Pénicaud L, Casteilla L, Lonchampt M, Dacquet C, Chavatte P, Berthelot P, Lesieur D.
    Journal: Bioorg Med Chem; 2006 Nov 15; 14(22):7377-91. PubMed ID: 16887353.
    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.
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