Novel C-2 Symmetric Molecules as α-Glucosidase and α-Amylase Inhibitors: Design, Synthesis, Kinetic Evaluation, Molecular Docking and Pharmacokinetics.

ABSTRACT: A series of symmetrical salicylaldehyde-bishydrazine azo molecules, 5a-5h, have been synthesized, characterized by ¹H-NMR and ¹³C-NMR, and evaluated for their in vitro α-glucosidase and α-amylase inhibitory activities. All the synthesized compounds efficiently inhibited both enzymes. Compound 5g was the most potent derivative in the series, and powerfully inhibited both α-glucosidase and α-amylase. The IC₅₀ of 5g against α-glucosidase was 0.35917 ± 0.0189 µM (standard acarbose IC₅₀ = 6.109 ± 0.329 µM), and the IC₅₀ value of 5g against α-amylase was 0.4379 ± 0.0423 µM (standard acarbose IC₅₀ = 33.178 ± 2.392 µM). The Lineweaver-Burk plot indicated that compound 5g is a competitive inh

SUBMITTER: Shahzad D 

PROVIDER: S-EPMC6515238 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature