Design and synthesis of new 1,2,3-triazole-methoxyphenyl-1,3,4-oxadiazole derivatives: selective butyrylcholinesterase inhibitors against Alzheimer's disease.

ABSTRACT: Alzheimer's disease (AD) remains a significant public health challenge due to its progressive cognitive impairment and the absence of proven treatments. In this study, several novel 1,2,3-triazole-methoxyphenyl-1,3,4-oxadiazole derivatives were synthesized and evaluated for their ability to inhibit key enzymes associated with AD: acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Structure-activity relationship (SAR) analysis revealed that derivatives featuring electron-withdrawing groups, particularly nitro and fluorine substituents, exhibited remarkable inhibitory activity against BChE while showing minimal effectiveness against AChE. Among these, compound 13s (R = 4-CH₃, R' = 4-NO₂) demonstrated the highest potency, selectively targeting BChE with an IC<

SUBMITTER: Iraji A 

PROVIDER: S-EPMC11998406 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature