57,344 results match your criteria cholinesterase inhibitors


A novel method of subxiphoid video-assisted thoracic surgery for thymectomy.

Ann Transl Med 2021 Aug;9(16):1339

Department of Thoracic Surgery, Fujian Medical University Union Hospital, Fuzhou, China.

Background: With advances in thoracoscopic surgical instruments and techniques, subxiphoid video-assisted thoracic surgery (S-VATS) has become the main approach for anterior mediastinal tumor resection under thoracoscopy. However, the drawbacks of S-VATS, including it being a relatively unfixed surgical procedure, make it complicated and difficult for unexperienced surgeons to master.

Methods: This study retrospectively reviewed and analyzed consecutive patients with anterior mediastinal tumor or myasthenia gravis (MG) who underwent S-VATS at the Fujian Medical University Union Hospital, China, between March 2015 and April 2019. Read More

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Design, synthesis, and bio-evaluation of new isoindoline-1,3-dione derivatives as possible inhibitors of acetylcholinesterase.

Res Pharm Sci 2021 Oct 19;16(5):482-492. Epub 2021 Aug 19.

Department of Animal Biotechnology, Cell Science Research Center, Royan Institute for Biotechnology, ACECR, Isfahan, I.R. Iran.

Background And Purpose: Alzheimer's disease is considered one of the lead causes of elderly death around the world. A significant decrease in acetylcholine level in the brain is common in most patients with Alzheimer's disease, therefore acetylcholinesterase (AChE) inhibitors such as donepezil and rivastigmine are widely used for patients with limited therapeutic results and major side effects.

Experimental Approach: A series of isoindoline-1,3-dione -N-benzyl pyridinium hybrids were designed, synthesized and evaluated as anti-Alzheimer agents with cholinesterase inhibitory activities. Read More

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October 2021

Persecution of Birds of Prey in Flanders: A Retrospective Study 2011-19.

J Wildl Dis 2021 Sep 13. Epub 2021 Sep 13.

Ghent University, Faculty of Veterinary Medicine, Department of Pathology, Bacteriology and Avian Diseases, Salisburylaan 133, 9820 Merelbeke, Belgium.

For decades birds of prey have been under the protection of European law, but deliberate or unintentional killing is still a large-scale problem in Europe. In an effort to monitor illegal practices, the Flemish government established several bird of prey hotlines in 2006. Since then, every suspicious death of a bird of prey has been investigated. Read More

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September 2021

Gender Disparities in Anti-dementia Medication Use among Older Adults: Health Equity Considerations and Management of Alzheimer's Disease and Related Dementias.

Front Pharmacol 2021 25;12:706762. Epub 2021 Aug 25.

Department of Pharmaceutical and Administrative Sciences, Presbyterian College School of Pharmacy, Clinton, SC, United States.

The prevalence of Alzheimer's disease and related dementias (ADRD) in women is higher than men. However, the knowledge of gender disparity in ADRD treatment is limited. Therefore, this study aimed to determine the gender disparities in the receipt of anti-dementia medications among Medicare beneficiaries with ADRD in the U. Read More

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CSF and Plasma Cholinergic Markers in Patients With Cognitive Impairment.

Front Aging Neurosci 2021 26;13:704583. Epub 2021 Aug 26.

Division of Clinical Geriatrics, Department of Neurobiology, Care Sciences and Society, Center for Alzheimer Research, Karolinska Institutet, Campus Flemingsberg, Stockholm, Sweden.

Introduction: Alzheimer's disease (AD) is the most prevalent form of dementia with symptoms of deteriorating cognitive functions and memory loss, partially as a result of a decrease in cholinergic neurotransmission. The disease is incurable and treatment with cholinesterase inhibitors (ChEIs) is symptomatic. Choline acetyltransferase (ChAT), the enzyme that synthesizes acetylcholine (ACh), has been proven recently to be present in both cerebrospinal fluid (CSF) and plasma. Read More

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Use of antipsychotic drugs and cholinesterase inhibitors and risk of falls and fractures: self-controlled case series.

BMJ 2021 09 9;374:n1925. Epub 2021 Sep 9.

School of Pharmacy, Institute of Clinical Pharmacy and Pharmaceutical Sciences, College of Medicine, National Cheng Kung University, Tainan, Taiwan

Objective: To evaluate the association between the use of antipsychotic drugs and cholinesterase inhibitors and the risk of falls and fractures in elderly patients with major neurocognitive disorders.

Design: Self-controlled case series.

Setting: Taiwan's National Health Insurance Database. Read More

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September 2021

Novel Sulfonamide-Based Carbamates as Selective Inhibitors of BChE.

Int J Mol Sci 2021 Aug 31;22(17). Epub 2021 Aug 31.

Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic.

A series of 14 target benzyl [2-(arylsulfamoyl)-1-substituted-ethyl]carbamates was prepared by multi-step synthesis and characterized. All the final compounds were tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in vitro, and the selectivity index (SI) was determined. Except for three compounds, all compounds showed strong preferential inhibition of BChE, and nine compounds were even more active than the clinically used rivastigmine. Read More

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First-in-Class Isonipecotamide-Based Thrombin and Cholinesterase Dual Inhibitors with Potential for Alzheimer Disease.

Molecules 2021 Aug 27;26(17). Epub 2021 Aug 27.

Department of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.

Recently, the direct thrombin (thr) inhibitor dabigatran has proven to be beneficial in animal models of Alzheimer's disease (AD). Aiming at discovering novel multimodal agents addressing thr and AD-related targets, a selection of previously and newly synthesized potent thr and factor Xa (fXa) inhibitors were virtually screened by the Multi-fingerprint Similarity Searching aLgorithm (MuSSeL) web server. The -phenyl-1-(pyridin-4-yl)piperidine-4-carboxamide derivative , which has already been experimentally shown to inhibit thr with a K value of 6 nM, has been flagged by a new, upcoming release of MuSSeL as a binder of cholinesterase (ChE) isoforms (acetyl- and butyrylcholinesterase, AChE and BChE), as well as thr, fXa, and other enzymes and receptors. Read More

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Acetylcholinesterase and butyrylcholinesterase inhibition by nectriapyrone and tryptophol isolated from endophytic fungus sp.

Nat Prod Res 2021 Sep 9:1-6. Epub 2021 Sep 9.

Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, Brazil.

Cholinesterase (ChE) inhibitors are currently the main drugs used to treat the cognitive symptoms of Alzheimer's disease (AD). Dual cholinesterase inhibitors, that is, compounds capable of inhibiting both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), are considered a new potential approach for the long-term treatment of patients with AD. We evaluated the ethyl acetate extract of sp. Read More

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September 2021

Assessment of Cholinesterase inhibition activity of birds inhabiting pesticide exposed croplands and protected area in hot semi-arid region of Pakistan.

Braz J Biol 2021 6;83:e248842. Epub 2021 Sep 6.

The University of Western Australia, School of Human Sciences, Perth, Australia.

Acetylcholinesterase (AChE) activity levels can be used as an indicator for AChE inhibition due to pesticide poisoning in bird species. We assessed the comparative brain cholinesterase (AChE) activity level of five bird species inhabiting pesticide exposed croplands and Protected Area i.e. Read More

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September 2021

A modified binary particle swarm optimization with a machine learning algorithm and molecular docking for QSAR modelling of cholinesterase inhibitors.

SAR QSAR Environ Res 2021 Sep;32(9):745-767

Department of Chemistry, Faculty of Science, University of Sistan and Baluchestan, Zahedan, Iran.

The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors play a key role in treating Alzheimer's disease. This study proposes an approach that integrates a modified binary particle swarm optimization (PSO) with a machine learning algorithm for building QSAR models to predict the activity of inhibitors for AChE and BuChE enzymes. More precisely, it uses a transfer function to convert the continuous search space of PSO to binary. Read More

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September 2021

MuSK Myasthenia Gravis Presenting with Bilateral Vocal Cord Abduction Paresis: A Case Report and Literature Review.

Neurologist 2021 Sep 7;26(5):175-177. Epub 2021 Sep 7.

Department of Neurology, Mayo Clinic, Rochester, MN.

Introduction: Approximately 39% to 49% of patients with previously diagnosed acetylcholine receptor antibody-negative myasthenia gravis have been found to be muscle-specific tyrosine kinase (MuSK) antibody positive. These patients have a presentation that typically includes oculobulbar weakness, poorer response to cholinesterase inhibitors, and higher risk for acute clinical decompensation that necessitates plasma exchange. MuSK patients can require more aggressive maintenance immunosuppression earlier-on to maintain stability, often with rituximab. Read More

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September 2021

Novel tacrine-based acetylcholinesterase inhibitors as potential agents for the treatment of Alzheimer's disease: Quinolotacrine hybrids.

Mol Divers 2021 Sep 7. Epub 2021 Sep 7.

Department of Medicinal Chemistry, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran.

A new series of quinolotacrine hybrids including cyclopenta- and cyclohexa-quinolotacrine derivatives were designed, synthesized, and assessed as anti-cholinesterase (ChE) agents. The designed derivatives indicated higher inhibitory effect on the acetylcholinesterase (AChE) with IC values of 0.285-100 µM compared to butyrylcholinesterase (BChE) with IC values of > 100 µM. Read More

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September 2021

A meta-analysis of randomised controlled trials of physical activity in people with Alzheimer's disease and mild cognitive impairment with a comparison to donepezil.

Int J Geriatr Psychiatry 2021 Oct 25;36(10):1471-1487. Epub 2021 May 25.

Department of Psychosis Studies, Institute of Psychiatry, Psychology & Neuroscience, King's College London, United Kingdom.

Objectives: Physical exercise may benefit people with Alzheimer's disease (AD) and mild cognitive impairment (MCI). However, randomised controlled trials (RCTs) of exercise have shown conflicting findings and it is unclear if positive outcomes are comparable to a commonly used cholinesterase inhibitor, donepezil.

Methods: Embase, Medline, PsycINFO, PsycARTICLES, SCOPUS were searched for RCTs of physical activity compared to a control condition, and donepezil compared to placebo in people with AD and MCI. Read More

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October 2021

[An effect of cholinesterase blockade on negative symptoms in schizophrenia].

Zh Nevrol Psikhiatr Im S S Korsakova 2021 ;121(8):37-44

Mental Health Research Center, Moscow, Russia.

Abstruct.

Objective: To assess the possibilities of influencing the severity of negative disorders in schizophrenic patients with cholinesterase blockade.

Material And Methods: The study included stable 26 patients (13 of them women), average age 40. Read More

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September 2021

Further SAR studies on natural template based neuroprotective molecules for the treatment of Alzheimer's disease.

Bioorg Med Chem 2021 Aug 28;46:116385. Epub 2021 Aug 28.

Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, India. Electronic address:

In our earlier paper, we described ferulic acid (FA) template based novel series of multifunctional cholinesterase (ChE) inhibitors for the management of AD. This report has further extended the structure-activity relationship (SAR) studies of this series of molecules in a calibrated manner to improve upon the ChEs inhibition and antioxidant property to identify the novel potent multifunctional molecules. To investigate the effect of replacement of phenylpiperazine ring with benzylpiperazine, increase in the linker length between FA and substituted phenyl ring, and replacement of indole moiety with tryptamine on this molecular template, three series of novel molecules were developed. Read More

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Dual monoamine oxidase and cholinesterase Inhibitors with different heterocyclic scaffolds.

Curr Top Med Chem 2021 Sep 2. Epub 2021 Sep 2.

Faculty of Pharmacy, Eastern Mediterranean University, Famagusta, T.R. North Cyprus, via Mersin 10 , Turkey.

For the last two decades, there has been research interest on the design of molecules possessing dual inhibitory potential on cholinesterase and monoamine oxidase enzymes, particularly for the treatment of two major neurodegenerative diseases, Alzheimer's disease (AD) and Parkinson's disease (PD). Many compounds have been synthesized for this purpose, and some of them have been shown to display activities comparable or superior to the activities of current drugs used for the treatment of AD and PD. Within the concept of this review study, we have aimed to present the current drugs used for the treatment of AD and PD, their mechanism of action, the discussion behind the theory of designing dual inhibitor agents, and the presentation of the most active compounds with diverse heterocyclic scaffolds displayed in research studies published in the recent period. Read More

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September 2021

European Stroke Organization and European Academy Neurology joint guidelines on post-stroke cognitive impairment.

Eur J Neurol 2021 Sep 3. Epub 2021 Sep 3.

Stroke Research group, Department of Clinical Neurosciences, University of Cambridge, Cambridge, UK.

Background And Purpose: The optimal management of post-stroke cognitive impairment (PSCI) remains controversial. These joint European Stroke Organization (ESO) and European Academy of Neurology (EAN) guidelines provide evidence-based recommendations to assist clinicians in decision making regarding prevention, diagnosis, treatment and prognosis.

Methods: Guidelines were developed according to the Grading of Recommendations, Assessment, Development and Evaluation (GRADE) methodology. Read More

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September 2021

Synthesis and characterization of a novel molecularly imprinted polymer for the controlled release of rivastigmine tartrate.

Mater Sci Eng C Mater Biol Appl 2021 Sep 24;128:112273. Epub 2021 Jun 24.

Center for Nanotechnology and Sustainability, Department of Mechanical Engineering, National University of Singapore, Singapore 117581, Singapore. Electronic address:

To develop novel imprinted poly (methacrylic acid) nanoparticles for the controlled release of Rivastigmine Tartrate (RVS), the amalgamation of molecular imprinting techniques and polymerization of precipitates were applied in this work. By permuting different concentrations of pentaerythritol triacrylate (PETA) or trimethylolpropane triacrylate (TMPTA) as cross-linkers, ten different samples were synthesized, and their abilities assessed for RVS absorption. Among them, uniform mono-disperse nanoparticles were synthesized in an RVS/PMAA/PETA mole ratio of 1:6:12, named molecularly imprinted polymers 2 (MIP2), which showed the highest RVS absorption. Read More

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September 2021

The Effect of Donepezil on Problem-solving Ability in Individuals With Amnestic Mild Cognitive Impairment: A Pilot Study.

Cogn Behav Neurol 2021 Sep 2;34(3):182-187. Epub 2021 Sep 2.

Departments of Neurology.

Background: Clinical trials involving individuals with mild cognitive impairment (MCI) have reported mixed results for the effects of cholinesterase inhibitors on cognitive outcomes. Our previous work demonstrated that a visuospatial problem-solving task was sensitive to non-memory impairments in individuals with MCI.

Objective: To determine whether the same task is also sensitive to the effects of cholinesterase inhibitors in individuals with amnestic MCI (aMCI). Read More

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September 2021

Neuroprotective derivatives of tacrine that target NMDA receptor and acetyl cholinesterase - Design, synthesis and biological evaluation.

Comput Struct Biotechnol J 2021 3;19:4517-4537. Epub 2021 Aug 3.

Molecular Neurobiology Division, Rajiv Gandhi Centre for Biotechnology, Thycaud PO, Thiruvananthapuram, Kerala 695014, India.

The complex and multifactorial nature of neuropsychiatric diseases demands multi-target drugs that can intervene with various sub-pathologies underlying disease progression. Targeting the impairments in cholinergic and glutamatergic neurotransmissions with small molecules has been suggested as one of the potential disease-modifying approaches for Alzheimer's disease (AD). Tacrine, a potent inhibitor of acetylcholinesterase (AChE) is the first FDA approved drug for the treatment of AD. Read More

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Source Attribution of the Chemical Warfare Agent Soman Using Position-Specific Isotope Analysis by H NMR Spectroscopy: From Precursor to Degradation Product.

Anal Chem 2021 09 1;93(36):12230-12236. Epub 2021 Sep 1.

Department of CBRN Defence & Security, The Swedish Defence Research Agency (FOI), Cementvägen 20, Umeå SE-901 82, Sweden.

Position-specific isotope analysis (PSIA) by NMR spectroscopy is a technique that provides quantitative isotopic values for every site-a so-called isotopic fingerprint-of a compound of interest. The isotopic fingerprint can be used to link samples with a common origin or to attribute a synthetic chemical to its precursor source. Despite PSIA by NMR being a powerful tool in chemical forensics, it has not yet been applied on chemical warfare agents (CWAs). Read More

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September 2021

A review on the microbial degradation of chlorpyrifos and its metabolite TCP.

Chemosphere 2021 Nov 6;283:131447. Epub 2021 Jul 6.

Institute of Environmental Sciences, Nguyen Tat Thanh University, Ho Chi Minh City, Viet Nam.

Chlorpyrifos (CPF) falls under the category of organophosphorus pesticides which are in huge demand in the agricultural sector. Overuse of this pesticide has led to the degradation of the quality of terrestrial and aquatic life. The chemical is moderately persistent in the environment but its primary metabolite 3,5,6-trichloro-2-pyridinol (TCP) is comparatively highly persistent. Read More

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November 2021

Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT receptor with anti-aggregation properties against amyloid-beta and tau.

Eur J Med Chem 2021 Aug 19;225:113783. Epub 2021 Aug 19.

Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland. Electronic address:

Multifunctional ligands as an essential variant of polypharmacology are promising candidates for the treatment of multi-factorial diseases like Alzheimer's disease. Based on clinical evidence and following the paradigm of multifunctional ligands we have rationally designed and synthesized a series of compounds targeting processes involved in the development of the disease. The biological evaluation led to the discovery of two compounds with favorable pharmacological characteristics and ADMET profile. Read More

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Plant-Based Synthesis of Zinc Oxide Nanoparticles (ZnO-NPs) Using Aqueous Leaf Extract of : Their Antiproliferative Activity against HepG2 Cells Inducing Reactive Oxygen Species and Other Properties.

Oxid Med Cell Longev 2021 17;2021:4786227. Epub 2021 Aug 17.

Department of Biotechnology, Quaid-i-Azam University, Islamabad 45320, Pakistan.

The anti-cancer, anti-aging, anti-inflammatory, antioxidant, and anti-diabetic effects of zinc oxide nanoparticles (ZnO-NPs) produced from aqueous leaf extract of were evaluated in this study. Several methods were used to characterize ZnO-NPs, including SEM, FTIR, XRD, DLS, PL, Raman, and HPLC. The nanoparticles that had a size of 34. Read More

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September 2021

Chemical composition and spectrum of insecticidal activity of the essential oils of Ocimumgratissimum L. and Cymbopogoncitratus Stapf on the main insects of the cotton entomofauna in Côte d'Ivoire.

Chem Biodivers 2021 Aug 27. Epub 2021 Aug 27.

Cotton Research Institute, Cotton Biology, Abidjan, Abidjan, COTE D'IVOIRE.

Among the alternatives to environmentally toxic and socio-economically unacceptable chemical pesticides, essential oils from Ocimum gratissimum and Cymbopogon citratus were tested on the main pests and beneficial insects of the cotton plant in Côte d'Ivoire. After extraction and chemical analysis of the essential oils, field trials were carried out using a Fisher block system with three treatment repetitions where their effects compared with those of a registered synthetic insecticide (IBIS A 52 EC). Foliar applications of the products were carried out in accordance with the cotton plant protection extension programme in Côte d'Ivoire from the 45th to the 115th day after plant emergence, with one application every fortnight. Read More

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Mitochondrial dysfunction and oxidative stress in liver of male albino rats after exposing to sub-chronic intoxication of chlorpyrifos, cypermethrin, and imidacloprid.

Pestic Biochem Physiol 2021 Oct 20;178:104938. Epub 2021 Jul 20.

Department of Pesticide Chemistry and Technology, Laboratory of Bioenergetics and Membrane Toxicology, Faculty of Agriculture, 21545-El-Shatby, Alexandria University, Alexandria, Egypt.

The adverse effects of chlorpyrifos, cypermethrin, and imidacloprid on mitochondrial dysfunction and oxidative stress biomarkers were studied in rat liver. The liver deficiency was also confirmed by histological analysis and gel electrophoresis. Each insecticide was administered orally with five doses per week for 28 days to male albino rats at 1/50 of the LD per insecticide. Read More

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October 2021

The insecticide chlorpyrifos modifies the expression of genes involved in the PXR and AhR pathways in the rainbow trout, Oncorhynchus mykiss.

Pestic Biochem Physiol 2021 Oct 14;178:104920. Epub 2021 Jul 14.

Laboratorio de Ecotoxicología Acuática, INIBIOMA- CONICET- CEAN, Ruta Provincial 61, Km 3, Junín de los Andes, Neuquén, Argentina. Electronic address:

Chlorpyrifos (CPF) is an organophosphate pesticide, commonly detected in water and food. Despite CPF toxicity on aquatic species has been extensively studied, few studies analyze the effects of CPF on fish transcriptional pathways. The Pregnane X receptor (PXR) is a nuclear receptor that is activated by binding to a wide variety of ligands and regulates the transcription of enzymes involved in the metabolism and transport of many endogenous and exogenous compounds. Read More

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October 2021

Effects of Microenvironmental Changes on the Fluorescence Signal of Alternariol: Magnesium Induces Strong Enhancement in the Fluorescence of the Mycotoxin.

Int J Mol Sci 2021 Aug 13;22(16). Epub 2021 Aug 13.

Department of Pharmacology, Faculty of Pharmacy, University of Pécs, Rókus u. 2, H-7624 Pécs, Hungary.

Alternariol (AOH) is an emerging mycotoxin produced by molds. It occurs as a contaminant e.g. Read More

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Quantum Calculations of VX Ammonolysis and Hydrolysis Pathways via Hydrated Lithium Nitride.

Int J Mol Sci 2021 Aug 11;22(16). Epub 2021 Aug 11.

Sandia National Laboratories, Albuquerque, NM 87185, USA.

Recently, lithium nitride (LiN) has been proposed as a chemical warfare agent (CWA) neutralization reagent for its ability to produce nucleophilic ammonia molecules and hydroxide ions in aqueous solution. Quantum chemical calculations can provide insight into the LiN neutralization process that has been studied experimentally. Here, we calculate reaction-free energies associated with the LiN-based neutralization of the CWA VX using quantum chemical density functional theory and ab initio methods. Read More

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