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  • Title: Synthesis, in vitro and in silico studies of a PPARγ and GLUT-4 modulator with hypoglycemic effect.
    Author: Navarrete-Vázquez G, Torres-Gómez H, Hidalgo-Figueroa S, Ramírez-Espinosa JJ, Estrada-Soto S, Medina-Franco JL, León-Rivera I, Alarcón-Aguilar FJ, Almanza-Pérez JC.
    Journal: Bioorg Med Chem Lett; 2014 Sep 15; 24(18):4575-4579. PubMed ID: 25131539.
    Abstract:
    Compound {4-[({4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy}acetyl)amino]phenoxy}acetic acid (1) was prepared and the in vitro relative expression of PPARγ, GLUT-4 and PPARα, was estimated. Compound 1 showed an increase of 2-fold in the mRNA expression of PPARγ isoform, as well as the GLUT-4 levels. The antidiabetic activity of compound 1 was determined at 50 mg/Kg single dose using a non insulin dependent diabetes mellitus (NIDDM) rat model. The in vivo results indicated a significant decrease of plasma glucose levels, during the 7 h post-administration. Also, we performed a molecular docking of compound 1 into the ligand binding pocket of PPARγ, showing important short contacts with residues Ser289, His323 and His449 in the active site.
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