Design, synthesis, and evaluation of triazolo[1,5-a]pyridines as novel and potent α‑glucosidase inhibitors.

ABSTRACT: α-Glucosidase is a key enzyme responsible for controlling the blood glucose, making a pivotal target in the treatment of type 2 diabetes mellitus. Present work introduces^1,2,4triazolo[1,5-a]pyridine as a novel, potent scaffold for α-glucosidase inhibition. A diverse scope of targeted compounds was prepared through an efficient, straightforward synthetic protocol. A series of compounds (15a-15v) were synthesized using a simple and efficient protocol, all showing notable inhibitory activity. Among them, compound 15j exhibited the best inhibition potency (IC₅₀ = 6.60 ± 0.09 µM), acting as a competitive and selective α-glucosidase inhibitor with no effect on α-amylase. Moreover, comprehensive computational studies were performed to validate the in vitro results and provide insight i

SUBMITTER: Peytam F 

PROVIDER: S-EPMC12098659 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature