New Tetrahydroacridine Hybrids with Dichlorobenzoic Acid Moiety Demonstrating Multifunctional Potential for the Treatment of Alzheimer's Disease.

ABSTRACT: A series of new tetrahydroacridine and 3,5-dichlorobenzoic acid hybrids with different spacers were designed, synthesized, and evaluated for their ability to inhibit both cholinesterase enzymes. Compounds 3a, 3b, 3f, and 3g exhibited selective butyrylcholinesterase (EqBuChE) inhibition with IC₅₀ values ranging from 24 to 607 nM. Among them, compound 3b was the most active (IC₅₀ = 24 nM). Additionally, 3c (IC₅₀ for EeAChE = 25 nM and IC₅₀ for EqBuChE = 123 nM) displayed dual cholinesterase inhibitory activity and was the most active compound against acetylcholinesterase (AChE). Active compound 3c was also tested for the ability to inhibit Aβ aggregation. Theoretical physicochemical properties of the

SUBMITTER: Czarnecka K 

PROVIDER: S-EPMC7312527 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature