RESUMEN

In this work, new derivatives of diarylimidazole-1,2,3-triazole 7a-p were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory activity. All compounds showed potent inhibitory activity in the range of IC50 = 90.4-246.7 µM comparing with acarbose as the standard drug (IC50 = 750.0 µM). Among the synthesized compounds, compounds 7b, 7c, and 7e were approximately 8 times more potent than acarbose. The kinetic study of those compounds indicated that they acted as the competitive inhibitors of α-glucosidase. Molecular docking studies were also carried out for compounds 7b, 7c, and 7e using modeled α-glucosidase to find the interaction modes responsible for the desired inhibitory activity.

Asunto(s)

Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Triazoles/química , Triazoles/farmacología , Diseño de Fármacos , Inhibidores de Glicósido Hidrolasas/síntesis química , Humanos , Imidazoles/síntesis química , Imidazoles/química , Imidazoles/farmacología , Modelos Moleculares , Simulación del Acoplamiento Molecular , Saccharomyces cerevisiae/enzimología , Triazoles/síntesis química , alfa-Glucosidasas/metabolismo