Design, Synthesis, and Evaluation of Novel 2H-Benzo[b][1,4]thiazin-3(4H)-one Derivatives as New Acetylcholinesterase Inhibitors.

ABSTRACT: Alzheimer's disease (AD) is a slowly progressive neurodegenerative disease that causes dementia in people aged 65 and over. In the present study, a series of thiadiazole hybrid compounds with benzothiazine derivatives as acetylcholinesterase inhibitors were developed and evaluated for their biological activity. The AChE and BChE inhibition potentials of all compounds were evaluated by using the in vitro Ellman method. The biological evaluation showed that compounds 3i and 3j displayed significant inhibitory activity against AChE. Compounds 3i and 3j showed IC₅₀ values of 0.027 µM and 0.025 µM against AChE, respectively. The reference drug donepezil (IC₅₀ = 0.021 µM) also showed significant inhibition against AChE. Further docking simulation

SUBMITTER: Haji Ali S 

PROVIDER: S-EPMC9000418 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature