A wide range of evidence show that acetylcholinesterase (AChE) inhibitors can interfere with the progression of Alzheimer's Disease (AD). The successful development of these compounds was based on a well-accepted theory that the decline in cognitive and mental functions associated with AD is related to the loss of cortical cholinergic neurotransmission. The earliest known AChE inhibitors, namel...

A series of tacrine-rhein hybrid compounds have been designed and synthesized as novel multifunctional potent ChE inhibitors. Most of the compounds inhibited ChEs in the nanomolar range in vitro effectively. Compound 10b was one of the most potent inhibitors and was 5-fold more active than tacrine toward AChE, and it also showed a moderate BuChE inhibition with an IC50 value of 200 nM. Kinetic ...

A virtual screening of the ZINC database was applied for the identification of novel cholinesterase inhibitors. The first step allowed to select compounds with favorable physicochemical properties. Then, the compounds were screened with the pharmacophore models built using crystal structures of donepezil, tacrine, decamethonium and bis-7-tacrine with acetylcholinesterase and well characterized ...

Abstract The condensation of tacrine aminopolymethylene derivatives with diethyl (ethoxymethylidene)malonate led to the new hybrid compounds—conjugates, which were effective inhibitors acetylcholinesterase (AChE) (IC 50 up 0.538 μM) and butyrylcholinesterase 0.0314 μM). They can displace propidium iodide from peripherical anionic site AChE at level reference drug donepezil demonstrate a weak an...

ABSTRACT. The electrochemical behavior of two chemically related acridine compounds: tacrine (TAC) and 9-aminoacridine (9-AA) was investigated on a hanging mercury drop electrode (HDME). study carried out by using Osteryoung square wave voltammetry (OSWV) cyclic (CV) techniques in the Britton-Robinson (B-R) buffer solution at pH = 2.0–12.0, KCl (0.1/0.2/0.3 M) methanol (0.0-50%) mixture as supp...

The aim of this review is to describe side effects of five antidementives which are approved by the United States Food and Drug Administration (FDA); four acetylcholinesterase inhibitors and one glutamate - or N-metyl-D-aspartat receptor antagonist - memantine. The antidementives are well tolerated and undesired effects are rare; except hepatotoxicity of tacrine and gastrointestinal side effect...

A wide range of evidence shows that acetylcholinesterase (AChE) inhibitors can interfere with the progression of Alzheimer's disease (AD). The successful development of these compounds was based on a well-accepted theory that the decline in cognitive and mental functions associated with AD is related to the loss of cortical cholinergic neurotransmission. The earliest known AChE inhibitors, name...

Following confinement to one chamber of a two-chamber exploration box (acquisition trial), male and female rats were intraperitoneally injected with saline, glucose (50, 100 mg/kg) or tacrine (1, 3 mg/kg). Twenty-four hours later they were given free access to this chamber and an identical novel one (retention trial). Tendencies to occupy the novel chamber (novelty-related location preferences)...