β-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. β-Lactams were synthesized from benzylidene-inden derivatives and acetoxyacetyl chloride. The inhibitory effect of these compounds was examined for human carbonic anhydrase I and II (hCA I, and II) and acetylcholinesterase (AChE). The results reveal that β-lactams are in...

A series of 7-hydroxycoumarin derivatives connected by an amidic linker to the different amines were designed and synthesized as cholinesterase inhibitors. Most compounds showed remarkable inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among them, N-(1-benzylpiperidin-4-yl)acetamide derivative 4r with IC50 value of 1.6 μM was the most potent compound ...

The potential anticholinesterase characteristics of some thiazole derivatives (2a–2j), including the 5-nitrothiophene moiety, were examined in this work. 1H-NMR, 13C-NMR, and HRMS spectral data used to determine structure compounds. Using a modified Ellman's spectrophotometric approach, each compound was tested for its ability inhibit acetylcholinesterase (AChE) butyrylcholinesterase (BuChE) en...

BACKGROUND Previous studies showed that acetylcholinesterase (AChE) activity is present in the downstream (arterial) part of the embryonic chick and rat heart, but its functional significance was unclear. To establish whether other components of a cholinergic signal-transduction pathway are present in the embryonic heart, we localised the mRNAs encoding choline acetyltransferase (ChAT), acetylc...

The mechanism of intoxication with organophosphorus compounds, including highly toxic nerve agents, is based on the irreversible inhibition of acetylcholinesterase that is followed by an accumulation of acetylcholine at peripheral and central cholinergic synapses, which in turn leads to the clinical manifestation of various signs and symptoms summarized as acute cholinergic crisis. Nerve agent ...

Besides its role in terminating acetylcholine-mediated neurotransmission, acetylcholinesterase (AChE) is found to be expressed and participate in the process of apoptosis in various cell types. However, the mechanisms underlying AChE up-regulation in neuronal cells remain elusive. Herein we demonstrated that glycogen synthase kinase-3beta (GSK3beta) mediates induced AChE-S expression during apo...

Inhibition of acetylcholinesterase (AChE), the key enzyme in the breakdown of acetylcholine, is considered as a promising strategy for the treatment of neurological disorders such as Alzheimer's disease, senile dementia, ataxia and myasthenia gravis. A potential source of AChE inhibitors is certainly provided by the abundance of plants in nature. This article aims to provide a comprehensive lit...

Acetylcholinesterase (AChE) that has been covalently inhibited by organophosphate compounds (OPCs), such as nerve agents and pesticides, has traditionally been reactivated by using nucleophilic oximes. There is, however, a clearly recognized need for new classes of compounds with the ability to reactivate inhibited AChE with improved in vivo efficacy. Here we describe our discovery of new funct...

Acetylcholinesterase (AChE) has been purified from three different regions of rat brain using Sephadex G 200 column. SDS PAGE (6%) showed single band for the purified AChE fractions. Purified and lyophilized AChE from different (NH4)2SO4 precipitated fractions of three brain parts were utilized for in vitro enzyme kinetics using Dimethoate (Dmt) as inhibitor. K(m) values for cerebellum and hypo...

Objective(s): The objective of this study was to evaluate pharmacological effect of Calligonum polygonoides against Krait snake’s venom acetylcholinesterase (AChE) and to extent it for the treatment of Alzheimer’s disease. Materials and Methods: Acetylcholinesterase activity was measured using Ellman method with some modification. The kinetic studies of methanolic extract of C. polygonoides aga...