The cattle tick, Rhipicephalus (Boophilus) microplus (Bm), and the sand fly, Phlebotomus papatasi (Pp), are disease vectors to cattle and humans, respectively. The purpose of this study was to characterize the inhibitor profile of acetylcholinesterases from Bm (BmAChE1) and Pp (PpAChE) compared to human and bovine AChE, in order to identify divergent pharmacology that might lead to selective in...

This work presents a novel fluorescent sensor for the determination of tacrine by combining the magnificent fluorescence properties of nitrogen-doped graphene quantum dots (N-GQDs) with the high potential of acetylcholinesterase (AChE) enzyme for screening its inhibitors. Tacrine was the first drug approved for Alzheimer's disease and it is currently being used in several therapeutic treatments...

O Cerrado brasileiro possui uma grande diversidade florística ainda pouco estudada sobre os efeitos e possíveis atividades biológicas de interesse humano, como a inibição da acetilcolinesterase (AChE). Extratos florais liofilizados diferentes espécies vegetais produzidos entre 2017-2022, mantidos -12 °C, foram utilizados. método utilizada, foi proposto por Ellman, modificado Miloševića colabora...

Nineteen tosylated acyl hydrazone derivatives were synthesized, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), β-secretase (BACE-1) evaluated. Compound 3o was the most potent inhibitor of MAO-A, with an IC50 value 1.54 µM, followed by 3a (IC50 = 3.35 µM). A structural comparison indicated that 3-F group in increased ...

Optimization of an essentially inactive 3,4-dihydro-2H-pyrano[3,2-c]quinoline carboxylic ester derivative as acetylcholinesterase (AChE) peripheral anionic site (PAS)-binding motif by double O → NH bioisosteric replacement, combined with molecular hybridization with the AChE catalytic anionic site (CAS) inhibitor 6-chlorotacrine and molecular dynamics-driven optimization of the length of the li...

Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) catalyze the hydrolysis of the neurotransmitter acetylcholine and, thereby, function as coregulators of cholinergic neurotransmission. For both enzymes, hydrolysis takes place near the bottom of a 20 Å deep active site gorge. A number of amino acid residues within the gorge have been identified as important in facilitating efficient ...

tacrine (9-amino-1,2,3,4-tetrahydroacridine) as a reversible inhibitor of acetylcholinesterase (ache),was the first drug for the symptomatic treatment of alzheimer’s disease (ad). nmr structuredetermination still presents some considerable challenges: the method is limited to systems ofrelatively small molecular mass, data collection times are long, data analysis remains a lengthyprocedure, and...

AIM The aim of this study was to characterize the pharmacokinetic and pharmacodynamic profile of donepezil HCl, a chemically distinct and specific acetylcholinesterase (AChE) inhibitor for the treatment of Alzheimer's disease, following administration of single oral doses. METHODS This was a double-blind, randomized, single-dose, placebo-controlled, sequential-group, ascending-dose study in h...

In a recent study, Blandizzi et al. (Br. J. Pharmacol., 132: 73 ± 84, 2001) reported that the adverse cholinergic e€ects of the chemotherapeutic agent irinotecan (CPT-11) were unlikely to be mediated by the inhibition of acetylcholinesterase (AChE). This observation was based on results of in vitro assays performed on AChE from two sources (human erythrocyte and electric eel). They reported onl...

The relative inhibitory potency (RIP) of an organophosphorus (OP) inhibitor against acetylcholinesterase (AChE) versus neuropathy target esterase (NTE) may be defined as the ratio [k(i)(AChE)/k(i)(NTE)], where k(i) is the bimolecular rate constant of inhibition for a given inhibitor against each enzyme. RIPs greater than 1 correlate with the inability of ageable OP inhibitors or their parent co...