Design, synthesis, and investigation of novel 5-arylpyrazole-glucose hybrids as α-glucosidase inhibitors.

ABSTRACT: Considering the global incidence of diabetes, developing new compounds to lower blood sugar levels has become increasingly crucial. As a result, there has been a growing focus on the synthesis of α-glucosidase inhibitors in recent years. This study investigated design, synthesis, and effects of novel 5-aryl pyrazole-glucose hybrids as α-glucosidase inhibitors. Thirteen derivatives from this class of compounds were synthesized, demonstrating superior in vitro inhibitory effects (IC₅₀ values ranging from 0.5 to 438.6 µM, compared to acarbose at 750.0 µM). Among them, compound 8g (IC₅₀ = 0.5 µM) was selected for further investigations and the kinetic studies revealed that it is a competitive inhibitor (K_i = 0.46 µM). Fluorescence assays indicated changes in th

SUBMITTER: Hariri R 

PROVIDER: S-EPMC11929827 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature