The purpose of the present work was to design, synthesize and screen in vitro, in vivo and in silico (in combo screens) a small series of five 3-[4-arylmethoxy)phenyl]propanoic acids to accomplish the treatment of diabetes with a single molecule with multitarget action: activation of PPARγ, GLUT-4 and GPR40 and inhibition of AKR1B1 (Figure 1). Here, AKR1B1 is linked to diabetes mellitus.