In our current research on antidiabetic compounds, we explain here the preparation of isobutyric acid derivatives 1–4 (Figure 1), their in vitro actions on PPARα/γ and GLUT-4 mRNA expression levels, the predictive biosimulations of their pharmacodynamics behavior and their in vivo effect in a murine model of diabetes. Here, SLC2A4 is linked to diabetes mellitus.