Synthesis of Novel 2,3-Dihydro-1,5-Benzothiazepines as α-Glucosidase Inhibitors: In Vitro, In Vivo, Kinetic, SAR, Molecular Docking, and QSAR Studies.

ABSTRACT: In the present study, a series of 2,3-dihydro-1,5-benzothiazepine derivatives 1B-14B has been synthesized sand characterized by various spectroscopic techniques. The enzyme inhibitory activities of the target analogues were assessed using in vitro and in vivo mechanism-based assays. The tested compounds 1B-14B exhibited in vitro inhibitory potential against α-glucosidase with IC₅₀ = 2.62 ± 0.16 to 10.11 ± 0.32 μM as compared to the standard drug acarbose (IC₅₀ = 37.38 ± 1.37 μM). Kinetic studies of the most active derivatives 2B and 3B illustrated competitive inhibitions. Based on the α-glucosidase inhibitory effect, the compounds 2B, 3B, 6B, 7B, 12B, 13B, and 1

SUBMITTER: Mehmood R 

PROVIDER: S-EPMC9435035 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature