Sergio Hidalgo-Figueroa, Juan J. Ramírez-Espinosa, Samuel Estrada-Soto, Julio C. Almanza-Pérez, Rubén Román-Ramos, Francisco J. Alarcón-Aguilar, Jesús V. Hernández-Rosado, Hermenegilda Moreno-Díaz, Daniel Díaz-Coutiño and Gabriel Navarrete-Vázquez Discovery of Thiazolidine-2,4-Dione/Biphenylcarbonitrile Hybrid as Dual PPAR α/γ Modulator with Antidiabetic Effect: In vitro, In Silico and In Vivo Approaches Chemical Biology & Drug Design 81
Article first published online: 21 MAR 2013 | DOI: 10.1111/cbdd.12102
Compound 1 was prepared using a short synthetic route. It showed an increase in the mRNA expression of PPARα and PPARγ, as well as the GLUT-4 levels. The antidiabetic activity of compound 1 was determined at 50 mg/kg single oral dose using a NIDDM rat model, showing a significant decrease in plasma glucose levels. Molecular docking of 1 into the ligand binding pocket of both PPAR´s isoforms showed important short contacts with the active PPARα and PPARγ residues.
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