Design, synthesis and α-glucosidase inhibition study of novel pyridazin-based derivatives

In this paper, pyridazin derivatives containing different thiobenzyl moieties were synthesized and screened for their inhibitory activities against rat intestinal α-glucosidase enzyme. The final products were easily obtained without the need to harsh purification steps. The in vitro results revealed that all the synthesized compounds were more potent (IC 50 s = 26.3–148.9 μM) than the clinically used drug, acarbose. The kinetic study revealed the competitive inhibition behavior of compound 5m (K i = −56 μM). Docking studies showed imperative interactions such as hydrogen bonding, Pi-Pi T-shaped, and Pi-anion interactions confirming the observed activity. The RMSD value was determined less than 3 Å and validated the study. Graphical Abstract