An article Enhancing insulin sensitivity by dual PPAR gamma partial agonist, beta-catenin inhibitor: Design, synthesis of new alpha phthalimido-o-toluoyl2-aminothiazole hybrids WOS:000579486500001 published article about 2-AMINOTHIAZOLE DERIVATIVES; ANTIVIRAL ACTIVITY; ALPHA; POTENT; DISCOVERY; ADIPOGENESIS; METABOLISM; BENZAMIDES; INDOLES; ACID in [Mourad, Ahmed A. E.] Port Said Univ, Fac Pharm, Pharmacol & Toxicol Dept, Port Said, Egypt; [Mourad, Mai A. E.] Port Said Univ, Fac Pharm, Med Chem Dept, Port Said, Egypt in 2020, Cited 42. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2. Recommanded Product: Isobenzofuran-1(3H)-one
Aims: Partial PPAR gamma agonists attracted substantially heightened interest as safer thiazolidinediones alternatives. On the other hand, Wnt/beta-catenin antagonists have been highlighted as promising strategy for type 2 diabetes management via up-regulating PPAR gamma gene expression. We aimed at synthesizing novel partial PPAR gamma agonists with beta-catenin inhibitory activity which could enhance insulin sensitivity and avoid the side effects of full PPAR gamma agonists. Main methods: We synthesized novel series of alpha-phthlimido-o-toluoyl-2-aminothiazoles hybrids for evaluating their antidiabetic activity and discovering its mechanistic pathway. We assessed effect of the new hybrids on PPAR gamma activation using a luciferase reporter assay system. Moreover, intracellular triglyceride levels, gene levels of c/EBP alpha, PPAR gamma and PPAR gamma targets including GLUT4, adiponectin, aP2 were measured in 3T3-L1 cells. Uptake of 2-DOG together with PPAR gamma and beta-catenin protein levels were evaluated in 3T3-L1cells. In addition, molecular docking studies with PPAR gamma LBD, physicochemical properties and structure activity relationship of the novel hybrids were also studied. Key findings: Three of the synthesized hybrids showed partial PPAR gamma agonistic activity and distinct PPAR gamma binding pattern. These compounds modulated PPAR gamma gene expression and PPAR gamma target genes; and increased glucose uptake in 3T3-L1 and slightly induced adipogenesis compared to rosiglitazone. Moreover, these compounds reduced beta-catenin protein level which reflected in increased both PPAR gamma gene and protein levels that leads to improved insulin sensitivity and increased GLUT4 and adiponectin gene expression. Significance: Our synthesized compounds act as novel partial PPAR gamma agonists and beta-catenin inhibitors that have potent insulin sensitizing activity and mitigate the lipogenic side effects of TZDs.
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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem