Alzheimer's disease (AD) is a multifactorial disorder with several target proteins contributing to its etiology. In search for multifunctional anti-AD drug candidates, taking into account that the acetylcholinesterase (AChE) and beta-amyloid (Aβ) aggregation are particularly important targets for inhibition, the tacrine and benzothiazole (BTA) moieties were conjugated with suitable linkers in a...

To simulate a convulsive syndrome, phenylcarbamate was administered intraperitoneally at dose of 1 mg/kg. Valproic acid aminoester (43 mg/kg), caramiphene (50 and diferidine (2 mg/kg) were investigated as potential anticonvulsant drugs. Blood brain tissue for the determination acetylcholinesterase (AСhE) taken 10, 30, 60 minutes, 6 24 hours after administration xenobiotic. In case poisoning wit...

In search of potent inhibitors cholinesterase enzymes and antioxidant agents, synthetic derivatives dihydroquinazolin-4(1H)-one 1-38 were evaluated as potential anti-Alzheimer agents through in vitro acetylcholinesterase (AChE) butyrylcholinesterase (BChE) inhibitions radical (DPPH ABTS) scavenging activities. The (SAR) was mainly based on the different substituents at aryl part which showed a ...

the effects of zinc and mercury on human erythrocyte acetylcholinestrase activity were studied. blood used in this study was obtained from 24 apparently healthy individuals and after hemolysation, was treted with 3 diferent concentrations of zinc and mercury. significant suppressions in acetylcholinestrase activity were recorded in treated samples by zinc and mercury. when compared to controls ...

Hemizygia bracteosa (Benth.) Briq (Lamiaceae) is used in the treatment of mental disease, memory loss, HIV, malaria and had antimicrobial and hypoglycemic properties. To the authors’ knowledge, no scientific study has been done on these properties except antimicrobial and hypoglycemic properties. The phytochemical investigation focused on the quantification of phenolic compounds, flavonoids, ta...

The complex nature of Alzheimer's disease calls for multidirectional treatment. Consequently, the search for multi-target-directed ligands may lead to potential drug candidates. The aim of the present study is to seek multifunctional compounds with expected activity against disease-modifying and symptomatic targets. A series of 15 drug-like various substituted derivatives of 2-(benzylamino-2-hy...

Acetylcholinesterase is involved in the termination of impulse transmission by rapid hydrolysis of the neurotransmitter acetylcholine in numerous cholinergic pathways in the central and peripheral nervous systems. The enzyme inactivation, induced by various inhibitors, leads to acetylcholine accumulation, hyperstimulation of nicotinic and muscarinic receptors, and disrupted neurotransmission. H...