231283-82-2

Upstream product

• 4803-57-0 2-(pyridin-4-yl)methyl-5,6-dimethoxy-1-indanone 
• 100-39-0 benzyl bromide 
• 877606-65-0 (E)-5, 6-dimethoxy-2-(pyridin-4-ylmethylene)-2, 3-dihydro-1H-inden-1-one 
• 2107-69-9 5,6-dimethoxy-1-indanone 
• 872-85-5 pyridine-4-carbaldehyde 

Relevant academic research and scientific papers

Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a "bio-Oxidizable" Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation

With the aim of reducing side effects of acetylcholinesterase inhibitors (AChEIs) during symptomatic treatment of Alzheimer's disease, we report herein a new class of donepezil-based "bio-oxidizable" prodrugs 1 designed to be converted into dual binding site AChEIs 2. While most of indanone-derived N-benzylpyridinium salts 2 revealed to be highly potent dual binding site hAChEIs (IC50 up to 3 nM), outperforming the standard drug donepezil (IC50 = 11 nM), most of the corresponding 1,4-dihydropyridines 1 were found to be inactive. Promisingly, whereas the selected prodrug 1r showed good permeability in the PAMPA-BBB model and high in vitro antioxidant activity, its conversion to AChEI 2r could be easily achieved under mild conditions when incubated in various oxidizing media. Lastly, both compounds 1r and 2r did not show genotoxicity in vitro and displayed high LD50 values in mice, making this prodrug 1r/drug 2r couple a good candidate for further in vivo biological experiments.

(1-INDANONE)-(1,2,3,6-TETRAHYDROPYRIDINE) DERIVATIVE

The present invention provides an excellent sigma receptor binding agent and/or acetylcholinesterase inhibitor containing an (1-indanone)-(1,2,3,6-tetrahydropyridine) compound. More specifically, it provides an (1-indanone)-(1,2,3,6-tetrahydropyridine) co

Acetylcholinesterase inhibitors containing 1-benzyl-pyridinium salts

The present invention provides an excellent acetylcholinesterase inhibitor. That is, it provides an acetylcholinesterase inhibitor comprising a 1-benzylpyridinium salt represented by the following formula: wherein R1, R2, R3 and R4 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitrile group, a C1-6 alkyl group, a C1-6 alkoxy group etc.; R5 represents a hydrogen atom, a halogen atom etc.; the partial structure: is a group represented by the formula >C(R6)—CH2— (wherein R6 is a hydrogen atom or a halogen atom) or >C═CH—; X?represents a halide ion or organic sulfonic acid ion; and m is 0 or an integer from 1 to 5.

Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block

A series benzylpiperidinium and benzylpyridinium quaternary salts have been synthesised and tested for inhibition of acetylcholinesterase and reversal of neuromuscular block induced by vecuronium. Several potent reversal agents have been identified and their haemodynamic effects measured.

Process for production of donepezil derivative

The present invention provides a novel industrially or economically preferable process for production of a hydrogen halogenide salt of a Donepezil derivative having an excellent pharmacological action as medicament, namely, reaction of 1-indanone derivative with carbonate ester to obtain 2-alkoxycarbonyl-1-indanone derivative, followed by reaction with halogenated (4-pyridyl)methyl or a salt thereof and decarboxylation successively to obtain 2-(4-pyridyl)methyl-1-indanone derivative, then reaction with halogenated benzyl to obtain quaternary ammonium salt, then reduction, and synthetic intermediates thereof. (Wherein R1represents a hydrogen atom or lower alkoxy; n represents an integer of 1 to 4; R2represents lower alkyl group; and X represents a halogen atom.)