Antioxidant and acetylcholinesterase inhibition activity of aliphatic and aromatic edaravone derivatives

Pyrazolone-type compounds (part II): in vitro and in silico evaluation of antioxidant potential; structure–activity relationship

“…The obtained results could be compared to other ndings, i.e., with compounds bearing pyrazolone fragment. 27,[56][57][58][59][60] Here, in comparison with the most similar edaravone-like set of compounds (and drug edaravone), 27 compounds a-t expressed signicantly higher antioxidant activity.…”

Some Aromatic Schiff Bases and Their Metal Complexes

“…Research has shown that aromatic carbonyl compounds form stable Schiff bases, while those with aliphatic compounds are prone to polymerization. Also, aromatic derivatives of some therapeutic agents were shown to be safer to use [5].…”

A protocol for directly accessing geminal C-4 diarylated pyrazol-5(4H)-ones via tandem C–H aryne insertion and their inceptive neurobiological evaluation

“…However, among the possible treatments for AD, acetylcholinesterase (AChE) inhibitors have received considerable attention because they provide symptomatic relief by compensating for the death of cholinergic neurons and restoring synaptic levels of the neurotransmitter. 11 Interestingly, AChE inhibitory assays have revealed that edaravone, an arylated pyrazolone, and its derivatives could be potent AChE inhibitors with therapeutic potential particularly because they exhibit good dipolarophilic affinity, 12 thereby facilitating blood-brain barrier (BBB) permeability to mediate neuroprotective and neurotrophic effects. It would thus appear that further aryl loading on the pyrazolone moiety, by leveraging the active C4-CH 2 unit, might open up unchartered, enriched therapeutic space for further scrutiny.…”