Chiral pyrimidinyl-piperazine carboxamide derivatives as potent yeast α-glucosidase inhibitors.

ABSTRACT: α-Glucosidase is an important target in treating type 2 diabetes, and thus, the inhibition of this enzyme could delay sugar digestion and avoid postprandial hyperglycemia. Previous studies revealed that some pyrimidine and piperazine derivatives showed good affinity towards α-glucosidase. In continuing efforts toward the development of α-glucosidase inhibitor, a series of pyrimidinyl-piperazine carboxamide 6-22 containing chiral center have been synthesized. The inhibition activity was evaluated against α-glucosidase from Saccharomyces cerevisiae. All tested compounds exhibit excellent inhibition effects compared to acarbose (IC₅₀ = 817.38 µM). Compounds bearing S-configurations at the chiral center displayed up to 5-fold more active than R-configurations. Among them, compounds

SUBMITTER: Herfindo N 

PROVIDER: S-EPMC12222516 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature