2010
DOI: 10.1248/cpb.58.1216
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Design, Synthesis and Evaluation of Difunctionalized 4-Hydroxybenzaldehyde Derivatives as Novel Cholinesterase Inhibitors

Abstract: A series of difunctionalized 4-hydroxybenzaldehyde derivatives were designed, synthesized and evaluated as cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)) inhibitors. The results demonstrated that all the compounds had more potent AChE and BChE inhibitory activities than galanthamine-HBr, one of the best cholinesterase inhibitors known so far. The inhibition mechanism revealed that the best active compound 4e displayed a mix-type mode of AChE and BChE by its dual-site interactions… Show more

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Cited by 6 publications
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“…The solvents were dried and purified before use. The aldehyde used for the synthesis of porphyrins was synthesized by following the previously reported procedure .…”
Section: Methodsmentioning
confidence: 99%
“…The solvents were dried and purified before use. The aldehyde used for the synthesis of porphyrins was synthesized by following the previously reported procedure .…”
Section: Methodsmentioning
confidence: 99%
“…4-HBA is a structural isomer of salicylaldehyde with one hydroxyl (-OH) group at the para position of the phenolic ring. Several studies have suggested that 4-HBA is an active candidate for improving insulin resistance and inhibiting cholinesterase 16 , 17 . However, the therapeutic effects of 4-HBA on acute wound healing have not been determined.…”
Section: Introductionmentioning
confidence: 99%