Discovery of Novel Pyrrolidine-Based Chalcones as Dual Inhibitors of α-Amylase and α-Glucosidase: Synthesis, Molecular Docking, ADMET Profiles, and Pharmacological Screening.

ABSTRACT: A series of chalcones containing a pyrrolidine moiety were synthesized to examine their in vitro α-amylase and α-glucosidase inhibitory activities, for the treatment of Diabetes mellitus, which is one of the most dangerous and rapidly increasing disorders of today. Compound 3 exhibited an excellent dual inhibitory effect with an IC₅₀ value of 14.61 ± 0.12 μM against α-amylase, and with an IC₅₀: 25.38 ± 2.09 μM against α-glucosidase. The in vitro cytotoxic effects of all compounds against nonsmall lung cancer (A549) and bronchial epithelial normal (BEAS-2B) cell lines were also evaluated. Compound 5 (IC₅₀: 82.20 μM) and compound 8 (IC₅₀: 59.96 μM) showed better cytotoxic activity than cisplatin against A54

SUBMITTER: Kursun Aktar BS 

PROVIDER: S-EPMC11904715 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature