A concept of tandem driven dynamic self-inhibition is demonstrated through dynamic inhibitors of acetylcholinesterase (AChE) using reversible transthiolesterification.

Myasthenia Gravis is autoimmune disorder of neuromuscular transmission. In some cases, psychiatric complications aggravate its course. Myasthenia gravis (MG) has always been a challenge for anesthesiologists and psychiatrists when the use of electroconvulsive therapy (ECT) is required, especially when succinylcholine is used together with acetylcholinesterase inhibitors. We describe a 76 years ...

BACKGROUND Acetylcholinesterase inhibitors are considered standard of care for Alzheimer's disease in many countries. Galantamine is an acetylcholinesterase inhibitor that may also act via allosteric modulation of nicotinic acetylcholine receptors. Therefore, it may provide benefits compared with other acetylcholinesterase inhibitors. The present study compared galantamine (n = 116) with donepe...

A matrix assisted laser desorption/ionization time-of-flight mass spectrometry platform for quantitatively monitoring enzyme activity and screening enzyme inhibitors has been demonstrated. The described method employs a new matrix of oxidized carbon nanotubes. Compared with the traditional fluorescence approach, this label-free method has the advantage of directly identifying the substrates and...

objective(s): alzheimer’s disease (ad) as progressive cognitive decline and the most common form of dementia is due to degeneration of the cholinergic neurons in the brain. therefore, administration of the acetylcholinesterase (ache) inhibitors such as donepezil is the first choice for treatment of the ad. in the present study, we focused on the synthesis and anti-cholinesterase evaluation of n...

A number of mono- and bis-quaternary ammonium salts, containing edrophonium-like and coumarin moieties tethered by an appropriate linker, proved to be highly potent and selective dual binding site acetylcholinesterase inhibitors with good selectivity over butyrylcholinesterase. Homobivalent bis-quaternary inhibitors 11 and 12, differing by only one methylene unit in the linker, were the most po...

Introduction: Acetylcholinesterase inhibitors constitute an effective class of drugs for the treatment of mild and moderate Alzheimer’s disease and are allowed by the responsible agencies for this purpose only. However, concrete evidence is still necessary in what concerns the impact of the use of such drugs to treat a large variety of cognitive disorders not classified as Alzheimer’sdi...