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Journal articles on the topic 'Cholinesterase Inhibitor'

Author: Grafiati

Published: 4 June 2021

Last updated: 26 July 2025

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1

Dehnabi, Manijeh, Açelya Mavideniz, Tugba Ercetin, and Hayrettin Ozan Gülcan. "Synthesis of 7-(3-(4-(2,3-dichlorophenyl)piperazin-1-yl)propoxy)-3,4-dihydroquinolin-2(1H)-one and Screening Its Cholinesterase Inhibitor Properties." EMU Journal of Pharmaceutical Sciences 8, no. 1 (2025): 8–13. https://doi.org/10.54994/emujpharmsci.1697699.

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Aripiprazole is a well-known atypical antipsychotic drug [i.e., 7-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-3,4-dihydroquinolin-2(1H)-one]. The pharmacological effects of aripiprazole are primarily attributed to its partial agonist activity at dopamine and serotonin receptors, although the exact mechanism of action remains unclear. However, it is generally accepted that aripiprazole exerts its therapeutic effects by modulating dopaminergic and serotoninergic neurotransmission. This study aimed to synthesize a modified derivative of aripiprazole and to investigate the cholinesterase inhi

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2

Smyrska-Wieleba, Natalia, and Tomasz Mroczek. "Natural Inhibitors of Cholinesterases: Chemistry, Structure–Activity and Methods of Their Analysis." International Journal of Molecular Sciences 24, no. 3 (2023): 2722. http://dx.doi.org/10.3390/ijms24032722.

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This article aims to provide an updated description and comparison of the data currently available in the literature (from the last 15 years) on the studied natural inhibitors of cholinesterases (IChEs), namely, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These data also apply to the likely impact of the structures of the compounds on the therapeutic effects of available and potential cholinesterase inhibitors. IChEs are hitherto known compounds with various structures, activities and origins. Additionally, multiple different methods of analysis are used to determine the cho

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3

Hwang, Jayeong, Kumju Youn, Yeongseon Ji, et al. "Biological and Computational Studies for Dual Cholinesterases Inhibitory Effect of Zerumbone." Nutrients 12, no. 5 (2020): 1215. http://dx.doi.org/10.3390/nu12051215.

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Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) mediate the degradation of acetylcholine (ACh), a primary neurotransmitter in the brain. Cholinergic deficiency occurs during the progression of Alzheimer’s disease (AD), resulting in widespread cognitive dysfunction and decline. We evaluated the potential effect of a natural cholinesterase inhibitor, zerumbone, using in vitro target enzyme assays, as well as in silico docking and ADMET (absorption, distribution, metabolism, excretion, and toxicity) simulation. Zerumbone showed a predominant cholinesterase inhibitory property with IC

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4

Coulson, Brett S., Brett S. Coulson, Stephen G. Fenner, and Osvaldo P. Almeida. "Successful Treatment of Behavioural Problems in Dementia Using a Cholinesterase Inhibitor: The Ethical Questions." Australian & New Zealand Journal of Psychiatry 36, no. 2 (2002): 259–62. http://dx.doi.org/10.1046/j.1440-1614.2002.00977.x.

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Objective: To review the effect of cholinesterase inhibitors on the behavioural and neuropsychiatric symptoms of dementia and discuss the current clinical guidelines for the prescription of cholinesterase inhibitors in Australia. Method: This paper reports the case of a patient with clinical diagnosis of dementia with lewy bodies (DLB) who was referred to an old age psychiatry service for the treatment of severe visual hallucinations and behavioural problems. Results: Pharmacological treatment with olanzapine produced marked parkinsonism, agitation and confusion. A cholinesterase inhibitor, do

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5

Chen, Yao, Yaoyao Bian, Yuan Sun, et al. "Identification of 4-aminoquinoline core for the design of new cholinesterase inhibitors." PeerJ 4 (July 7, 2016): e2140. http://dx.doi.org/10.7717/peerj.2140.

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Inhibition of acetylcholinesterase (AChE) using small molecules is still one of the most successful therapeutic strategies in the treatment of Alzheimer’s disease (AD). Previously we reported compound T5369186 with a core of quinolone as a new cholinesterase inhibitor. In the present study, in order to identify new cores for the designing of AChE inhibitors, we screened different derivatives of this core with the aim to identify the best core as the starting point for further optimization. Based on the results, we confirmed that only 4-aminoquinoline (compound 04 and 07) had cholinesterase inh

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6

Koay, Yee-Hui, Alireza Basiri, Vikneswaran Murugaiyah, and Kit-Lam Chan. "Isocorilagin, a Cholinesterase Inhibitor from Phyllanthus niruri." Natural Product Communications 9, no. 4 (2014): 1934578X1400900. http://dx.doi.org/10.1177/1934578x1400900423.

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Drugs that have dual inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) produce better clinical efficacy against Alzheimer's disease (AD) than those that selectively inhibit one enzyme. A dual cholinesterase inhibitory-guided fractionation of Phyllanthus niruri leaves afforded isocorilagin, a bioactive tannin possessing good inhibitory activities against AChE (IC50: 0.49 μM) and BChE (IC50: 4.20 μM). Interestingly, isocorilagin was relatively 2- to 3-fold more potent than galanthamine, the clinically used inhibitor. The kinetic analyses suggested that isocorilagin was a

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7

Petroianu, G. A., A. Schmitt, K. Arafat, and M. Y. Hasan. "Weak Inhibitors Protect Cholinesterases from Stronger Inhibitors (Dichlorvos): In Vitro Effect of Tiapride." International Journal of Toxicology 24, no. 2 (2005): 79–86. http://dx.doi.org/10.1080/10915810590921360.

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Metoclopramide is a benzamide dopamine receptor antagonist and serotonine receptor agonist widely used as an antiemetic and gastric prokinetic drug. In addition, metoclopramide is a weak and reversible inhibitor of cholinesterases. The authors have previously shown that metoclopramide has a cholinesterase protective effect against inhibition by organophosphates (OPs). The putative mode of protective action of metoclopramide is, when administered in excess, competion for the active site of the enzyme with the more potent OP. In the present paper the authors present their results using another b

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Nordberg, Agneta, Taher Darreh-Shori, Elaine Peskind, et al. "Different Cholinesterase Inhibitor Effects on CSF Cholinesterases in Alzheimer Patients." Current Alzheimer Research 6, no. 1 (2009): 4–14. http://dx.doi.org/10.2174/156720509787313961.

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9

Knuepfer, Mark M., and Qi Gan. "Role of cholinergic receptors and cholinesterase activity in hemodynamic responses to cocaine in conscious rats." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 276, no. 1 (1999): R103—R112. http://dx.doi.org/10.1152/ajpregu.1999.276.1.r103.

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It has been suggested that toxicity to cocaine is related to the relative rate of cocaine metabolism by cholinesterases and to activation of cholinergic receptors either directly or by reflex mechanisms. We examined these possibilities by altering cholinesterase activity and blocking cholinergic receptors in rats prone or resistant to cocaine-induced cardiovascular toxicity. Rats were instrumented with a pulsed Doppler flow probe on the ascending aorta for measurement of cardiac output and cannulated for arterial pressure and heart rate determination. In conscious rats, cocaine (5 mg/kg iv) el

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10

Mlakić, Milena, Ivan Faraho, Ilijana Odak, et al. "Cholinesterase Inhibitory and Anti-Inflammatory Activity of the Naphtho- and Thienobenzo-Triazole Photoproducts: Experimental and Computational Study." International Journal of Molecular Sciences 24, no. 19 (2023): 14676. http://dx.doi.org/10.3390/ijms241914676.

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New 1,2,3-triazolo(thieno)stilbenes were synthesized as mixtures of isomers and efficiently photochemically transformed to their corresponding substituted thienobenzo/naphtho-triazoles in high isolated yields. The resulting photoproducts were studied as acetyl- (AChE) and butyrylcholinesterase (BChE) inhibitors without or with interconnected inhibition potential of TNF-α cytokine production. The most promising anti-inflammatory activity was shown again by naphtho-triazoles, with a derivative featuring 4-pentenyl substituents exhibiting notable potential as a cholinesterase inhibitor. To identi

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11

Khadka, Sandhya, Rajesh Basnet, Sandeep Shrestha, Yuchun Wang, and Radheshyam Gupta. "Acetyl cholinesterase: a potential target for Alzheimer’s disease intervention." Journal of Patan Academy of Health Sciences 7, no. 2 (2020): 95–97. http://dx.doi.org/10.3126/jpahs.v7i2.31130.

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Alzheimer's disease is a neurological disorder in which the death of brain cells causes memory loss and cognitive decline. The role of treatment is not limited to pharmacology, but also involves many factors, such as the psychological, social, and economic aspects of the patient and family. It is important to consider the use of AChe inhibitors in patients with mild to moderate AD, despite cost issues and in the absence of any other immediate progression. Although there are allots of currently available inhibitor for acetyl cholinesterase but there is no selective potent inhibitor for AD. so,

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Saleh, Solin, Andrew Kirk, Debra G. Morgan, and Chandima Karunanayake. "Less Education Predicts Anticholinesterase Discontinuation in Dementia Patients." Canadian Journal of Neurological Sciences / Journal Canadien des Sciences Neurologiques 40, no. 5 (2013): 684–90. http://dx.doi.org/10.1017/s031716710001492x.

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Abstract:Objective:We investigated patient socio-demographic, clinical and functional factors predicting cholinesterase inhibitor discontinuation by patients presenting to a memory clinic in Saskatoon, Saskatchewan.Methods:Data collection began in March 2004 at the Rural and Remote Memory Clinic where family physicians referred their non-institutionalized patients. Neurological and neuropsychological assessment, patient and caregiver questionnaires provided the socio-demographic, clinical and functional variables. Univariate logistic regression analysis was used to examine possible association

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13

Misra, Biswapriya B., and Satyahari Dey. "TLC-Bioautographic Evaluation of In Vitro Anti-tyrosinase and Anti-cholinesterase Potentials of Sandalwood Oil." Natural Product Communications 8, no. 2 (2013): 1934578X1300800. http://dx.doi.org/10.1177/1934578x1300800231.

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Sandalwood oil, rich in sesquiterpenoid alcohols, has been used in traditional medicinal systems as a relaxant and coolant. Besides, sandalwood oil is used as an ingredient in numerous skin fairness enhancing cosmetics. However, there is no available information on biological activities that relate to the above applications. Hence, the anti-tyrosinase and anti-cholinesterase potentials of sandalwood oil were probed by both TLC-bioautographic and colorimetric methods. Results obtained from colorimetric assays indicated that sandalwood oil is a potent inhibitor of tyrosinase (IC50=171 μg mL−1) a

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14

GONZALEZ ROTHI, LESLIE J., RENEE FULLER, SUSAN A. LEON, et al. "Errorless practice as a possible adjuvant to donepezil in Alzheimer’s disease." Journal of the International Neuropsychological Society 15, no. 2 (2009): 311–22. http://dx.doi.org/10.1017/s1355617709090201.

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AbstractSix individuals with probable Alzheimer’s disease (AD) participated in a phase 1 study employing a repeated measures, parallel baseline design testing the hypothesis that error-free experience during word production practice combined with an acetyl cholinesterase inhibitor would improve confrontation naming ability. While acetyl cholinesterase inhibitors are safe and delay cognition decline associated with AD, improvement over baseline cognition is less evident; clinically significant cognitive deficits persist and progress. Both animal and clinical research strongly implicate acetylch

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15

Komatović, Katarina, Ana Matošević, Nataša Terzić-Jovanović, et al. "4-Aminoquinoline-Based Adamantanes as Potential Anticholinesterase Agents in Symptomatic Treatment of Alzheimer’s Disease." Pharmaceutics 14, no. 6 (2022): 1305. http://dx.doi.org/10.3390/pharmaceutics14061305.

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Considering that acetylcholinesterase (AChE) inhibition is the most important mode of action expected of a potential drug used for the treatment of symptoms of Alzheimer’s disease (AD), our previous pilot study of 4-aminoquinolines as potential human cholinesterase inhibitors was extended to twenty-two new structurally distinct 4-aminoquinolines bearing an adamantane moiety. Inhibition studies revealed that all of the compounds were very potent inhibitors of AChE and butyrylcholinesterase (BChE), with inhibition constants (Ki) ranging between 0.075 and 25 µM. The tested compounds exhibited a m

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16

Kos, Jiri, Violetta Kozik, Dominika Pindjakova, et al. "Synthesis and Hybrid SAR Property Modeling of Novel Cholinesterase Inhibitors." International Journal of Molecular Sciences 22, no. 7 (2021): 3444. http://dx.doi.org/10.3390/ijms22073444.

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A library of novel 4-{[(benzyloxy)carbonyl]amino}-2-hydroxybenzoic acid amides was designed and synthesized in order to provide potential acetyl- and butyrylcholinesterase (AChE/BChE) inhibitors; the in vitro inhibitory profile and selectivity index were specified. Benzyl(3-hydroxy-4-{[2-(trifluoromethoxy)phenyl]carbamoyl}phenyl)carbamate was the best AChE inhibitor with the inhibitory concentration of IC50 = 36.05 µM in the series, while benzyl{3-hydroxy-4-[(2-methoxyphenyl)carbamoyl]phenyl}-carbamate was the most potent BChE inhibitor (IC50 = 22.23 µM) with the highest selectivity for BChE (

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17

Pohanka, Miroslav. "Postponed effect of neostigmine on oxidative homeostasis." Interdisciplinary Toxicology 7, no. 3 (2014): 134–38. http://dx.doi.org/10.2478/intox-2014-0018.

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ABSTRACT Cholinesterases are enzymes able to hydrolyze the neurotransmitter acetylcholine and thus to terminate transmission. Once the enzymes are inhibited, excitotoxicity can appear in the adjacent cells. It is well known that oxidative stress is involved in the toxicity of cholinesterase inhibitors. Commonly, stress follows inhibition of cholinesterases and disappears shortly afterwards. In the present experiment, it was decided to test the impact of an inhibitor, neostigmine, on oxidative stress in BALB/c mice after a longer interval. The animals were sacrificed three days after onset of t

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18

Gawel, Kinga, Krzysztof Labuz, Ewa Gibula-Bruzda, et al. "Acquisition and reinstatement of ethanol-induced conditioned place preference in rats: Effects of the cholinesterase inhibitors donepezil and rivastigmine." Journal of Psychopharmacology 30, no. 7 (2016): 676–87. http://dx.doi.org/10.1177/0269881116642539.

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The present study examined the influence of the cholinesterase inhibitors donepezil (a selective inhibitor of acetylcholinesterase) and rivastigmine (also an inhibitor of butyrylcholinesterase) on the acquisition and reinstatement of ethanol-induced conditioned place preference (CPP) in rats. Before the CPP procedure, animals received a single injection of ethanol (0.5 g/kg, 10% w/v, intraperitoneally [i.p.]) for 15 days. The ethanol-induced CPP (biased method) was developed by four injections of ethanol (0.5 g/kg, 10% w/v, i.p.) every second day. Control rats received saline instead of ethano

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Zdražilová, Pavla, Šárka Štĕpánková, Alena Komersová, Martina Vránová, Karel Komers, and Alexander Čegan. "Kinetics of 13 New Cholinesterase Inhibitors." Zeitschrift für Naturforschung C 61, no. 7-8 (2006): 611–17. http://dx.doi.org/10.1515/znc-2006-7-823.

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Kinetics of hydrolysis of acetylcholine and acetylthiocholine by two types of acetylcholinesterase and butyrylcholinesterase inhibited by 13 new inhibitors (5 carbamates and 8 carbazates - hydrazinium derivatives) was measured in vitro in a batch reactor at 25 °C, pH 8, ionic strength 0.11 ᴍ and enzyme activity 3.5 U by four nondependent analytical methods. Sevin®, rivastigmin (Exelon®) and galantamin (Reminyl®) served as comparative inhibiting standards. Kinetics of hydrolyses inhibited by all studied carbamates, sevin, carbazates (with exceptions) and rivastigmin (with exceptions) can be sim

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de Almeida, Raquel B. M., Deyse B. Barbosa, Mayra R. do Bomfim, et al. "Identification of a Novel Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase: In Vitro and In Silico Studies." Pharmaceuticals 16, no. 1 (2023): 95. http://dx.doi.org/10.3390/ph16010095.

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The enhancement of cholinergic functions via acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition is considered a valuable therapeutic strategy for the treatment of Alzheimer’s disease. This study aimed to evaluate the in vitro effect of ZINC390718, previously filtered using computational approaches, on both cholinesterases and to characterize, using a molecular dynamics (MD) simulation, the possible binding mode of this compound inside the cholinesterase enzymes. The in vitro cytotoxicity effect was also investigated using a primary astrocyte-enriched glial cell culture. Z

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Hwang, Jayeong, Kumju Youn, Gyutae Lim, Jinhyuk Lee, Dong Hyun Kim, and Mira Jun. "Discovery of Natural Inhibitors of Cholinesterases from Hydrangea: In Vitro and In Silico Approaches." Nutrients 13, no. 1 (2021): 254. http://dx.doi.org/10.3390/nu13010254.

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Alzheimer’s disease (AD) is a neurodegenerative disease conceptualized as a clinical-biological neurodegenerative construct where amyloid-beta pathophysiology is supposed to play a role. The loss of cognitive functions is mostly characterized by the rapid hydrolysis of acetylcholine by cholinesterases including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Moreover, both enzymes are responsible for non-catalytic actions such as interacting with amyloid β peptide (Aβ) which further leads to promote senile plaque formation. In searching for a natural cholinesterase inhibitor, the

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22

Kachhadiya, Radhika, Denish Prajapati, Krishna Patel, and Navnit Prajapati. "Synthesis and Virtual Screening of Some Novel Quinazolinone Derivatives as Potent Cholinesterase Inhibitors against Alzheimer’s Disease." Journal of Drug Delivery and Therapeutics 12, no. 5 (2022): 20–27. http://dx.doi.org/10.22270/jddt.v12i5.5625.

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In the past few decades, the cholinergic theory of Alzheimer's disease has been promoted as a crucial tool for the creation of new drugs. In this study, a series of novel quinazolinone scaffold were synthesized, docked and predicted for their ADMET studies for cholinesterase inhibitors against Alzheimer’s disease. Docking study were performed, using Autodock 4.2 for the synthesized compounds 4a-c and were observed to be well accommodated in the active site of AChE compared to standard Donepezil. Compounds 4d-f were most suggested novel quinazolinone derivative that the inhibitor exhibited two

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Štĕpánková, Šárka, Karel Komers, Alena Komersová, Markéta Masopustová, and Alexander Čegan. "Inhibition of Cholinesterase by Dialkylcarbamates." Zeitschrift für Naturforschung C 62, no. 3-4 (2007): 308–10. http://dx.doi.org/10.1515/znc-2007-3-423.

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Abstract The pI50 index and separation coefficients of chosen 3-N,N-diethylaminophenyl-N′,N′-dialkylcarbamates were determined. Index pI50 (pI50 = negative logarithm of molar concentration of inhibitor inhibiting the enzyme activity by 50%) describes the effectiveness of the inhibitor. The rate of ability of the inhibitor to pass the blood-brain barrier is usually described by the separation coefficient in a system n-octanol/water (Kow). Obtained results were compared with pI50 and Kow of Exelon®, the commercially used drug against the Alzheimer’s disease.

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Ramírez-Sánchez, Karla, Fernando Alvarado-Hidalgo, Inés Ardao, and Ricardo Starbird-Pérez. "Enzymatic Inhibition Constant of Acetylcholinesterase for the Electrochemical Detection and Sensing of Chlorpyrifos." Journal of Natural Resources and Development 8 (February 20, 2018): 09–14. http://dx.doi.org/10.5027/jnrd.v8i0.02.

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Infiltration into soils of pesticides used during agricultural production has led to the contamination of aquatic ecosystems due to their long persistence in the environment. Some pesticides (e.g. Chlorpyrifos) are inhibitors of cholinesterase enzyme activity and their presence in water samples can be indirectly detected by a decrease in enzymatic activity. Biosensors based on cholinesterase enzymes are an alternative for the sensitive detection of important contaminants in the environmental sector. Acetylcholinesterase enzyme (AChE) catalyzes the hydrolysis of acetylthiocholine (ATCh) to prod

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Hayashi, K., T. Hamano, R. Asano, et al. "Reduction of serum cholinesterase by cholinesterase inhibitor (Donepezil, Galantamine, or Rivastigmine)." Journal of the Neurological Sciences 381 (October 2017): 329–30. http://dx.doi.org/10.1016/j.jns.2017.08.936.

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Leikin, Jerrold B., Victoria Braund, and Carol DesLauris. "Cholinergic symptoms with low serum cholinesterase from therapeutic cholinesterase inhibitor toxicity." American Journal of Emergency Medicine 32, no. 7 (2014): 815.e3–815.e4. http://dx.doi.org/10.1016/j.ajem.2013.12.048.

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Sun, In O., Hyun Ju Yoon, and Kwang Young Lee. "Prognostic Factors in Cholinesterase Inhibitor Poisoning." Medical Science Monitor 21 (2015): 2900–2904. http://dx.doi.org/10.12659/msm.894287.

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Wagle, Kamal C., Becky Natali, and George E. Taffet. "Cholinesterase Inhibitor Initiation in Hospital Setting." Journal of the American Geriatrics Society 59, no. 10 (2011): 1988–89. http://dx.doi.org/10.1111/j.1532-5415.2011.03610_19.x.

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SHERMAN, K. A., and E. MESSAMORE. "CHOLINESTERASE INHIBITOR THERAPY FOR ALZHEIMER DEMENTIA." Alzheimer Disease & Associated Disorders 2, no. 3 (1988): 216. http://dx.doi.org/10.1097/00002093-198802030-00065.

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Richards, Lisa. "Cholinesterase inhibitor use link with syncope." Nature Reviews Neurology 5, no. 7 (2009): 350. http://dx.doi.org/10.1038/nrneurol.2009.83.

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SEIMIYA, Yukio, Takehiro FURUKAWA, Maki TAKAHASHI, et al. "Cholinesterase Inhibitor Poisoning in Wild Birds." Journal of the Japan Veterinary Medical Association 60, no. 3 (2007): 191–95. http://dx.doi.org/10.12935/jvma1951.60.191.

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ABBRECHT, P. H., R. R. KYLE, and H. J. BRYANT. "Pulmonary Mechanical Responses to Cholinesterase Inhibitor." Toxicological Sciences 13, no. 3 (1989): 593–604. http://dx.doi.org/10.1093/toxsci/13.3.593.

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ABBRECHT, P. "Pulmonary mechanical responses to cholinesterase inhibitor." Fundamental and Applied Toxicology 13, no. 3 (1989): 593–604. http://dx.doi.org/10.1016/0272-0590(89)90297-2.

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BRUNK, DOUG. "‘Poor’ Data Support Cholinesterase Inhibitor Use." Clinical Neurology News 3, no. 3 (2007): 17. https://doi.org/10.1016/s1553-3212(07)70090-0.

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Fadaeinasab, Mehran, Alireza Basiri, Yalda Kia, Hamed Karimian, Hapipah Mohd Ali, and Vikneswaran Murugaiyah. "New Indole Alkaloids from the Bark of Rauvolfia Reflexa and their Cholinesterase Inhibitory Activity." Cellular Physiology and Biochemistry 37, no. 5 (2015): 1997–2011. http://dx.doi.org/10.1159/000438560.

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Background/Aims: Rauvolfia reflexa is a member of the Apocynaceae family. Plants from the Apocynaceae family have been traditionally used in the treatment of age-related brain disorders Methods and Results: Two new indole alkaloids, rauvolfine C (1) and 3-methyl-10,11-dimethoxy-6-methoxycarbonyl-β-carboline (2), along with five known, macusine B (3), vinorine (4), undulifoline (5), isoresrpiline (6) and rescinnamine (7) were isolated from the bark of Rauvolfia reflexa. Cholinesterase inhibitory assay and molecular docking were performed to get insight of the inhibitory activity and molecular i

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Heise, Niels V., Jördis-Ann Schüler, Torje E. Orlamünde, et al. "Triterpenoid cholinesterase inhibitors that might improve gait disturbances in Parkinson's disease patients." Mediterranean Journal of Chemistry 12, no. 2 (2022): 188. http://dx.doi.org/10.13171/mjc02211021650csuk.

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:<strong> </strong>Parkinson's disease (PD) is the second most common neurodegenerative disease. Besides rigidity and tremor, patients often suffer from gait disturbance. Treatment with cholinesterase inhibitors (ChEI) has been shown to improve gait speed. Thus, the triterpene acids oleanolic acid and ursolic acid have been used as starting materials for the synthesis of compounds intended to act as inhibitors of the enzymes acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The parent compounds were acetylated and converted via isocyanates and amines into a series of am

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Ungvarská Maľučká, Lucia, and Jozef Csöllei. "Design, Synthesis and Biological Activity of New Carbamate Cholinesterase Inhibitors." Chemické listy 116, no. 6 (2022): 372–80. http://dx.doi.org/10.54779/chl20220372.

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The work deals with the design, synthesis and biological activity of new carbamate cholinesterase inhibitors. It is focused on selected syntheses of new carbamate derivatives, which were tested for their anticholinesterase activity against acetylcholinesterase as well as butyrylcholinesterase. Despite various theories in the pathogenesis of Alzheimer's disease, drugs that can inhibit these two enzymes still represent the major approach to the treatment of this neurodegenerative disease. Many of the newly synthesized compounds have unique chemical structure. Recently, the approach to the synthe

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Sobow, Tomasz, Marcin Flirski, Pawel Liberski, and And Kloszewska. "Plasma Ab levels as predictors of response to rivastigmine treatment in Alzheimer's disease." Acta Neurobiologiae Experimentalis 67, no. 2 (2007): 131–39. http://dx.doi.org/10.55782/ane-2007-1640.

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Cholinesterase inhibitors are currently the mainstream of symptomatic treatment of patients with Alzheimer's disease. The response to treatment with cholinesterase inhibitors is clinically difficult to predict. Several demographic, clinical and biological variables have been proposed as pretreatment predictors of long-term therapy efficacy. In this paper, consistently with previous reports, we confirm that higher initial disease severity and faster progression of cognitive impairment increase the chance of a clinically meaningful response to cholinesterase inhibitor therapy in a carefully sele

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Biscussi, Brunella, Victoria Richmond, Carlos Javier Baier, Pau Arroyo Mañez, and Ana Paula Murray. "Design and Microwave-Assisted Synthesis of Aza-Resveratrol Analogs with Potent Cholinesterase Inhibition." CNS & Neurological Disorders - Drug Targets 19, no. 8 (2020): 630–41. http://dx.doi.org/10.2174/1871527319666200905121536.

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Background: Currently approved Alzheimer’s disease medications mainly comprise acetylcholinesterase inhibitors. Many of these inhibitors are either natural compounds or synthetic molecules inspired in natural compounds. Hybrid molecules that can interact with different target sites of the enzyme could lead to the discovery of effective multitarget drugs. Objective: To design, synthesize, and evaluate a series of new aza-resveratrol analogs as in vitro acetyl- and butyrylcholinesterase inhibitors. Methods: The synthesis is achieved by a simple and efficient microwave-assisted method, from comme

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Sichaem, Jirapast, Santi Tip-pyang, and Kiattisak Lugsanangarm. "Bioactive Aporphine Alkaloids from the Roots of Artabotrys spinosus: Cholinesterase Inhibitory Activity and Molecular Docking Studies." Natural Product Communications 13, no. 10 (2018): 1934578X1801301. http://dx.doi.org/10.1177/1934578x1801301011.

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Six aporphine alkaloids (1–6) were isolated from Artabotrys spinosus roots based on bioassay-guided fraction and chromatographic methods. All isolated alkaloids were evaluated for their cholinesterase (ChEs) inhibitory activities, in which compounds 4 and 6 exhibited the highest activity toward butyrylcholinesterase (BChE) and acetylcholinesterase (AChE), respectively. The Lineweaver-Burk plots suggested that 4 and 6 were mixed mode inhibitors toward BChE and AChE enzymes, respectively. In addition, the experimental results were also confirmed by molecular docking analysis. This information ca

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Delogu, Giovanna Lucia, Michela Bengala, Maria João Matos, et al. "A New Class of Benzo[b]thiophene-chalcones as Cholinesterase Inhibitors: Synthesis, Biological Evaluation, Molecular Docking and ADME Studies." Molecules 29, no. 16 (2024): 3748. http://dx.doi.org/10.3390/molecules29163748.

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In this study, heterocyclic compounds containing a benzothiophene scaffold were designed and synthetized, and their inhibitory activity against cholinesterases (ChE) and the viability of SH-SY5Y cells have been evaluated. Benzothiophenes 4a–4i and benzothiophene-chalcone hybrids 5a–5i were tested against both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), revealing interesting structure–activity relationships. In general, benzothiophene–chalcone hybrids from series 5 proved to be better inhibitors of both enzymes, with compound 5f being the best AChE inhibitor (IC50 = 62.10 μM)

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Herrmann, Nathan. "Cognitive Pharmacotherapy of Alzheimer's Disease and other Dementias." Canadian Journal of Psychiatry 47, no. 8 (2002): 715–22. http://dx.doi.org/10.1177/070674370204700802.

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Objective: The objective of this paper is to review the randomized controlled trials (RCTs) on the pharmacotherapy of Alzheimer's disease and other dementias and to provide evidence-based recommendations for treatment of the cognitive impairment associated with these disorders. Method: A Medline search was conducted for RCTs, using the following key words: Alzheimer's disease, dementia, therapy, cholinesterase inhibitor, donepezil, rivastigmine, and galantamine. Studies were critically appraised, followed by a review of published major clinical practice guidelines. Recommendations for treatmen

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Gaustad, R., K. Sletten, D. Løvhaug, and F. Fonnum. "Purification and characterization of carboxylesterases from rat lung." Biochemical Journal 274, no. 3 (1991): 693–97. http://dx.doi.org/10.1042/bj2740693.

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Carboxylesterase (EC 3.1.1.1) has played an important part in our understanding of the toxicokinetic behaviour of the organophosphorus cholinesterase inhibitors. Carboxylesterases are a heterogeneous group of enzymes that can be separated on the basis of their isoelectric points and by their substrate-specificity. We have purified the isoenzyme (pI 5.8) present in greatest activity in rat lung to near homogeneity. The enzyme was purified by (NH4)2SO4 precipitation, gel filtration, chromatofocusing, separation on anion- and cation-exchangers and hydrophobic-interaction chromatography. The purif

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Clayton, Bridgette A., Ken-ichiro Hayashida, Steven R. Childers, Ruoyu Xiao, and James C. Eisenach. "Oral Donepezil Reduces Hypersensitivity after Nerve Injury by a Spinal Muscarinic Receptor Mechanism." Anesthesiology 106, no. 5 (2007): 1019–25. http://dx.doi.org/10.1097/01.anes.0000265163.22007.6d.

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Background Cholinesterase inhibitors which reach the central nervous system produce pain relief but are poorly tolerated because of gastrointestinal side effects. Here, the authors tested whether donepezil, a central nervous system penetrant cholinesterase inhibitor with a low incidence of gastrointestinal side effects, would relieve hypersensitivity in an animal model of neuropathic pain. Methods Male rats were anesthetized, and the L5 and L6 spinal nerves were ligated unilaterally. Hypersensitivity was measured by withdrawal threshold to von Frey filament application to the hind paw after or

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Herrmann, Nathan, Carin Binder, William Dalziel, Steve Smyth, and Fernando Camacho. "Persistence with Cholinesterase Inhibitor Therapy for Dementia." Drugs & Aging 26, no. 5 (2009): 403–7. http://dx.doi.org/10.2165/00002512-200926050-00004.

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Wilde, V. De, J. Vandenbogaerde, and W. Buylaert. "Acute Cholinesterase Inhibitor Poisoning Mimicking Pulmonary Oedema." Acta Clinica Belgica 44, no. 2 (1989): 133–36. http://dx.doi.org/10.1080/17843286.1989.11718001.

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Okazaki, Tatsuma, Katsutoshi Furukawa, Hiroshi Kubo, et al. "PARALYTIC ILEUS AFTER DISCONTINUATION OF CHOLINESTERASE INHIBITOR." Journal of the American Geriatrics Society 54, no. 10 (2006): 1620–21. http://dx.doi.org/10.1111/j.1532-5415.2006.00896.x.

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Holmstedt, Bo, Lennart Krook, and James R. Rooney. "The Pathology of Experimental Cholinesterase-Inhibitor Poisoning." Acta Pharmacologica et Toxicologica 13, no. 4 (2009): 337–44. http://dx.doi.org/10.1111/j.1600-0773.1957.tb00269.x.

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Patterson, C., and D. B. Hogan. "Brief Review: Rivastigmine, A Second Cholinesterase Inhibitor." Canadian Journal of Neurological Sciences / Journal Canadien des Sciences Neurologiques 28, S1 (2001): S122—S123. http://dx.doi.org/10.1017/s0317167100001293.

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Veloso, Anthony J., Paul M. Nagy, Biao Zhang, et al. "Miniaturized electrochemical system for cholinesterase inhibitor detection." Analytica Chimica Acta 774 (April 2013): 73–78. http://dx.doi.org/10.1016/j.aca.2013.02.033.

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