Design, synthesis, and evaluation of 3,7-substituted coumarin derivatives as multifunctional Alzheimer's disease agents.

ABSTRACT: Multitarget directed ligands (MTDLs) are emerging as promising treatment options for Alzheimer's disease (AD). Coumarin derivatives serve as a good starting point for designing MTDLs due to their inherent inhibition of monoamine oxidase (MAO) and cholinesterase enzymes, which are complicit in AD's complex pathophysiology. A preliminary series of 3,7-substituted coumarin derivatives were synthesised and evaluated for enzyme inhibitory activity, cytotoxicity as well as neuroprotective ability. The results indicated that the compounds are weak cholinesterase inhibitors with five compounds demonstrating relatively potent inhibition and selectivity towards MAO-B with IC₅₀ values between 0.014 and 0.498 hx00B5;µM. Significant neuroprotective effects towards MPP⁺-compromised

SUBMITTER: Mzezewa SC 

PROVIDER: S-EPMC8291583 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature