On October 15, 2020, Mourad, Ahmed A. E.; Mourad, Mai A. E. published an article.Category: thiazole The title of the article was Enhancing insulin sensitivity by dual PPARγ partial agonist, β-catenin inhibitor: Design, synthesis of new α-phthalimido-o-toluoyl-2-aminothiazole hybrids. And the article contained the following:
We aimed at synthesizing novel partial PPARγ agonists with β-catenin inhibitory activity which was enhanced insulin sensitivity and avoid the side effects of full PPARγ agonists. We synthesized novel series of α-phthlimido-o-toluoyl-2-aminothiazoles I [R1=R2=R3=R4 = H; R2 = H, Me, MeO, Cl, etc.] hybrids for evaluating their antidiabetic activity and discovering its mechanistic pathway. We assessed effect of the new hybrids I on PPARγ activation using a luciferase reporter assay system. Moreover, intracellular triglyceride levels, gene levels of c/EBPα, PPARγ and PPARγ targets including GLUT4, adiponectin, aP2 were measured in 3T3-L1 cells. Uptake of 2-DOG together with PPARγ and β-catenin protein levels were evaluated in 3T3-L1cells. In addition, mol. docking studies with PPARγ LBD, physicochem. properties and structure activity relationship of the novel hybrids I were also studied. Three of the synthesized hybrids I showed partial PPARγ agonistic activity and distinct PPARγ binding pattern. These compounds I modulated PPARγ gene expression and PPARγ target genes; and increased glucose uptake in 3T3-L1 and slightly induced adipogenesis compared to rosiglitazone. Moreover, these compounds I reduced β-catenin protein level which reflected in increased both PPARγ gene and protein levels that leads to improved insulin sensitivity and increased GLUT4 and adiponectin gene expression. This synthesized compounds act as novel partial PPARγ agonists and β-catenin inhibitors that have potent insulin sensitizing activity and mitigate the lipogenic side effects of TZDs. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Category: thiazole
The Article related to dioxoisoindolinylmethyl phenylthiazolyl benzamide preparation peroxisome proliferator activated receptor agonist, 2-aminothiazole, partial pparγ agonist, thiazolidinediones, wnt/β-catenin inhibitor, α-phthlimido-o-toluoyl and other aspects.Category: thiazole
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica