The present study reports the synthesis of a series N-substituted derivatives of brominated 2-phenitidine. First, the reaction of 2-phenitidine (1) with benzenesulfonyl chloride (2) in aqueous media yielded N-(2-ethoxyphenyl) benzenesulfonamide (3), which was then subjected to bromination with bromine in the presence of glacial acetic acid to give N-(4,5-dibromo-2-ethoxyphenyl)benzenesulfonamid...

BACKGROUND/AIM Traditional risk factors, like impaired transmitral flow in diastolic filling [vortex formation time (VFT) as echocardiographic parameter], contribute to Alzheimer's disease (AD). Moreover, we observed that acetylcholinesterase inhibitors provide a significant cardioprotection. We assessed the pathogenetic role of VFT as early cardiovascular risk factor in 23 AD patients and 24 c...

organophosphorus compounds are known to inhibit the esteratic site of acetylcholinesterase by phosphorylation. the phosphorylated esteratic site of acetylcholinesterase undergoes hydrolytic regeneration at a slow or negligible rate. nucleophilic agents such as hydroxytamine, hydroxamic acids, and oximes reactivate the enzyme more erapidfy than does spontaneous hydrolysis. the red cell cholinest...

Observations with acetylcholinesterase can be well explained by postulating that the active site contains two subsites: one, an anionic site which binds and orients substituted ammonium ions, and the other, an esteratic site where the hydrolytic process occurs and which contains a basic group which is acetylated and deacetylated during the process (4, 5). The formation of an acetyl enzyme sugge...

BACKGROUND Cognitive Stimulation Therapy (CST) is effective and cost-effective for people with mild-to-moderate dementia when delivered biweekly over 7 weeks. AIMS To examine whether longer-term (maintenance) CST is cost-effective when added to usual care. METHODS Cost-effectiveness analysis within multicenter, single-blind, pragmatic randomized controlled trial; subgroup analysis for peopl...

We report a randomized, double-blind, parallel group, placebo-controlled study to test the effects of the acetylcholinesterase inhibitor, donepezil (5 mg/d for 30 days), on aircraft pilot performance in 18 licensed pilots with mean age of 52 years. After 30 days of treatment, the donepezil group showed greater ability to retain the capacity to perform a set of complex simulator tasks than the p...

New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compar...

A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman's method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showe...

There is increasing evidence suggesting that the use of acetylcholinesterase inhibitors may have beneficial effects on bone. Data on the potential post-surgical effects of these medications on orthopedic interventions are very limited. This study was designed to determine whether the use of acetylcholinesterase inhibitors is associated with a decrease in post-surgical mortality and complication...

Factors such as oxidative stress and reduced acetylcholine level have been implicated in Alzheimer’s disease (AD) pathology and recently there has been a trend towards natural product research to find potential sources of antioxidants and acetylcholinesterase inhibitors in the plants kingdom. Centaurea is a genus with about 500 species world wild, many of them have shown to possess bio...