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Cholinesterase inhibitors

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https://www.readbyqxmd.com/read/27923619/synthesis-and-application-of-%C3%AE-carbolines-as-novel-multi-functional-anti-alzheimer-s-disease-agents
#1
William Horton, Abha Sood, Swarada Peerannawar, Nandor Kugyela, Aditya Kulkarni, Rekha Tulsan, Chris D Tran, Jessica Soule, Harry LeVine, Béla Török, Marianna Török
The design, synthesis and assessment of β-carboline core-based compounds as potential multifunctional agents against several processes that are believed to play a significant role in Alzheimer's disease (AD) pathology, are described. The activity of the compounds was determined in Aβ self-assembly (fibril and oligomer formation) and cholinesterase (AChE, BuChE) activity inhibition, and their antioxidant properties were also assessed. To obtain insight into the mode of action of the compounds, HR-MS studies were carried out on the inhibitor-Aβ complex formation and molecular docking was performed on inhibitor-BuChE interactions...
November 24, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27918993/tetrahydropyranodiquinolin-8-amines-as-new-non-hepatotoxic-antioxidant-and-acetylcholinesterase-inhibitors-for-alzheimer-s-disease-therapy
#2
Youssef Dgachi, Olga Sokolov, Vincent Luzet, Justyna Godyń, Dawid Panek, Alexandre Bonet, Hélène Martin, Isabel Iriepa, Ignacio Moraleda, Cristina García-Iriepa, Jana Janockova, Lysiane Richert, Ondrej Soukup, Barbara Malawska, Fakher Chabchoub, José Marco-Contelles, Lhassane Ismaili
Herein we report an efficient two step synthesis and biological assessment of 12 racemic tetrahydropyranodiquinolin-8-amines derivatives as antioxidant, cholinesterase inhibitors and non-hepatotoxic agents. Based on the results of the primary screening, we identified 7-(3-methoxyphenyl)-9,10,11,12-tetrahydro-7H-pyrano[2,3-b:5,6-h']diquinolin-8-amine (2h) as a particularly interesting non-hepatotoxic compound that shows moderate antioxidant activity (1.83 equiv Trolox in the ORAC assay), a non competitive inhibition of hAChE (IC50 = 0...
November 23, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27913252/sex-and-gender-differences-in-the-treatment-of-alzheimer-s-disease-a-systematic-review-of-randomized-controlled-trials
#3
Marco Canevelli, Federica Quarata, Francesca Remiddi, Flaminia Lucchini, Eleonora Lacorte, Nicola Vanacore, Giuseppe Bruno, Matteo Cesari
In recent years, epidemiological, clinical, and biological evidence has drawn the attention on the influence of sex and gender on Alzheimer's disease (AD). Nevertheless, not enough attention has been paid to their impact on treatment outcomes. The present study is aimed at systematically retrieve, review and discuss data coming from available randomized placebo-controlled trials (RCTs) on currently marketed treatments for AD (i.e., cholinesterase inhibitors [ChEIs] and memantine) in order to describe possible sex and gender differences in their efficacy, safety and tolerability...
November 30, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27913166/dose-dependent-effect-of-donepezil-administration-on-long-term-enhancement-of-visually-evoked-potentials-and-cholinergic-receptor-overexpression-in-rat-visual-cortex
#4
Mira Chamoun, Marianne Groleau, Menakshi Bhat, Elvire Vaucher
Stimulation of the cholinergic system tightly coupled with periods of visual stimulation boosts the processing of specific visual stimuli via muscarinic and nicotinic receptors in terms of intensity, priority and long-term effect. However, it is not known whether more diffuse pharmacological stimulation with donepezil, a cholinesterase inhibitor, is an efficient tool for enhancing visual processing and perception. The goal of the present study was to potentiate cholinergic transmission with donepezil treatment (0...
November 29, 2016: Journal of Physiology, Paris
https://www.readbyqxmd.com/read/27911327/anticholinergic-exposure-and-risk-of-pneumonia-in-persons-with-alzheimer-s-disease-a-nested-case-control-study
#5
Pasi Lampela, Anna-Maija Tolppanen, Antti Tanskanen, Jari Tiihonen, Sirpa Hartikainen, Heidi Taipale
BACKGROUND: Risk of pneumonia is increased in persons with Alzheimer's disease (AD). In some studies, anticholinergic drugs (AC) have been associated with an increased pneumonia risk. OBJECTIVE: We analyzed the risk of pneumonia associated with ACs in persons with AD. METHODS: We performed a nested case-control study using register-based data from a Finnish nationwide MEDALZ cohort including all community-dwelling persons diagnosed with AD during 2005-2011...
November 28, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/27911323/short-term-response-is-not-predictive-of%C3%A2-long-term-response-to%C3%A2-acetylcholinesterase-inhibitors-in-old-age-subjects-with-alzheimer-s-disease-a%C3%A2-real-world-study
#6
Virginia Boccardi, Marta Baroni, Nicoletta Smirne, Alessandra Clodomiro, Sara Ercolani, Annalisa Longo, Carmelinda Ruggiero, Amalia C Bruni, Patrizia Mecocci
BACKGROUND: Most of clinical guidelines recommend discontinuing treatment with cholinesterase inhibitors (ChEIs) in patients with Alzheimer's disease (AD) who do not show an initial response to therapy as evaluated with the Mini-Mental State Examination (MMSE) scale. However, understanding the relationship between the initial response to ChEI treatment and the subsequent course of the disease is extremely important in clinical practice, but evidence is limited, particularly in the old-old population...
November 29, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/27911310/cholinergic-modification-of-neurogenesis-and-gliosis-improves-the-memory-of%C3%A2-a%C3%AE-ppswe-psen1de9-alzheimer-s-disease-model-mice-fed-a-high-fat-diet
#7
Takeshi Matsuda, Tatsuhiro Hisatsune
We previously reported that neuroinflammation contributes to the amnesia of AβPPswe/PSEN1dE9 Alzheimer's disease model mice fed a high-fat diet to induce type-2 diabetes (T2DM-AD mice), but the underlying mechanism for the memory decline remained unclear. Recent studies have suggested that cholinergic modulation is involved in neuroinflammatory cellular reactions including neurogenesis and gliosis, and in memory improvement. In this study, we administered a broad-spectrum cholinesterase inhibitor, rivastigmine (2 mg/kg/day, s...
November 28, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/27910192/novel-tacrine-based-pyrano-3-4-5-6-pyrano-2-3-b-quinolinones-synthesis-and-cholinesterase-inhibitory-activity
#8
Roshanak Hariri, Zahra Afshar, Mohammad Mahdavi, Maliheh Safavi, Mina Saeedi, Zahra Najafi, Reyhaneh Sabourian, Elahe Karimpour-Razkenari, Najmeh Edraki, Farshad Homayouni Moghadam, Abbas Shafiee, Mahnaz Khanavi, Tahmineh Akbarzadeh
In order to develop effective anti-cholinesterase compounds, a novel series of pyrano[3',4':5,6]pyrano[2,3-b]quinolinones were designed, synthesized, and evaluated in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). All derivatives showed very good AChE inhibitory (AChEI) activity (IC50  = 0.37-5.62 μM) compared with rivastigmine (IC50  = 11.07 μM). Among them, 11-amino-12-(2,3-dichlorophenyl)-3-methyl-7,8,9,10-tetrahydropyrano[3',4':5,6]pyrano[2,3-b]quinolin-1(12H)-one (6f) displayed the best inhibitory activity...
December 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27907966/getting-rid-of-weakness-in-the-icu-an-updated-approach-to-the-acute-management-of-myasthenia-gravis-and-guillain-barr%C3%A3-syndrome
#9
Alexis A Lizarraga, Karlo J Lizarraga, Michael Benatar
After prompt diagnosis, severe myasthenia gravis and Guillain-Barré syndrome (GBS) usually require management in the intensive care unit. In the myasthenic patient, recognition of precipitating factors is paramount, and frequent monitoring of bulbar, upper airway, and/or respiratory muscle strength is needed to identify impending myasthenic crisis. Noninvasive ventilation can be attempted prior to intubation and mechanical ventilation in the setting of respiratory failure. Cholinesterase inhibitors should be discontinued, but resumed prior to extubation, and steroid dosage could be increased once the airway is secured...
December 2016: Seminars in Neurology
https://www.readbyqxmd.com/read/27906438/cholinesterase-inhibitors-and-non-steroidal-anti-inflammatory-drugs-as-alzheimer-s-disease-therapies-an-updated-umbrella-review-of-systematic-reviews-and-meta-analyses
#10
C-H Wang, L-S Wang, N Zhu
OBJECTIVE: Alzheimer's Disease (AD) is a major neurological disorder marked by an amyloid-beta plaque and neurofibrillary tau-tangle depositions in the brain. Cognitive dysfunction is the key manifestation of AD. In this study, we conducted an umbrella review of meta-analyses on the risk factors and therapeutics targeting cognitive impairment and AD. MATERIALS AND METHODS: We searched PubMed from January 2000-August, 2016, and screened systematic reviews and meta-analyses of studies that examined the effects of cholinesterase inhibitors in AD patients...
November 2016: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/27890007/a-current-perspective-on-the-inhibition-of-cholinesterase-by-natural-and-synthetic-inhibitors
#11
Anzer A Shah, Showkat A Ganie, Mohammad A Kamal, Tanveer Ali Dar
Majority of the observed cognitive and behavioral changes in Alzheimer's diseaseare postulated to be due to the deficiencies in cholinergic pathways of the brain. Enhancement of cholinergic transmission may thus stimulate the cholinergic receptors or prolong the availability of acetylcholine in synaptic cleft and hence improve the Alzheimer's disease associated symptoms. Of these two, the inhibition of cholinesterases (Acetylcholinesterase and Butyrylcholinesterase) by cholinesterase inhibitors is suggested to be a promising strategy...
November 23, 2016: Current Drug Metabolism
https://www.readbyqxmd.com/read/27885575/administration-of-huperzia-quadrifariata-extract-a-cholinesterase-inhibitory-alkaloid-mixture-has-neuroprotective-effects-in-a-rat-model-of-cerebral-hypoxia-ischemia
#12
F K Odorcyk, E F Sanches, F C Nicola, J Moraes, L F Pettenuzzo, J Kolling, C Siebert, A Longoni, E L Konrath, A Wyse, C A Netto
Neonatal hypoxia-ischemia (HI) is an etiologic component of several neurologic pathologies associated to cognitive impairment. The mechanisms involved in HI-induced tissue damage start immediately after HI and extend for days. Acetylcholine is an important neurotransmitter in the central nervous system and exerts a protector effect on tissue damage by modulating inflammation, and cholinesterase inhibitors have shown neuroprotective properties and their action are often attributed to inhibition of the immune response...
November 24, 2016: Neurochemical Research
https://www.readbyqxmd.com/read/27876467/a-review-on-tacrine-based-scaffolds-as-multi-target-drugs-mtdls-for-alzheimer-s-disease
#13
REVIEW
Bilqees Sameem, Mina Saeedi, Mohammad Mahdavi, Abbas Shafiee
Alzheimer's disease (AD) is a multifactorial neurological disorder among elderly people and combinatorial factors such as genetic, lifestyle, and environmental are involved in onset and disease progression. It has been demonstrated that loss of cholinergic transmission is one of the most significant causes of AD. One strategy currently being investigated for the development of new therapeutics relates to the enhancement of cholinergic system through several ways. At this juncture, anticholinesterase inhibitors have absorbed lots of attention and different marketed drugs such as donepezil, rivastigmine, tacrine, and galantamine have been developed...
October 28, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27865835/cholinesterases-inhibition-and-molecular-modeling-studies-of-piperidyl-thienyl-and-2-pyrazoline-derivatives-of-chalcones
#14
Muhammad Shakil Shah, Shafi Ullah Khan, Syeda Abida Ejaz, Saifullah Afridi, Syed Umar Farooq Rizvi, Muhammad Najam-Ul-Haq, Jamshed Iqbal
Super-activation of cholinesterases (acetylcholinesterase and butyrylcholinesterase) are linked to various neurological problems most precisely Alzheimer's disease (AD), which leads to senile dementia. Therefore, cholinesterases (AChE & BChE) inhibition are considered as a promising strategy for the treatment of Alzheimer's disease. FDA approved drugs for the treatment of AD, belong to a group of cholinesterase inhibitors. However, none of them is able to combat or completely abrogate the disease progression...
November 16, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27865771/cholinergic-activation-affects-the-acute-and-chronic-antinociceptive-effects-of-morphine
#15
Kinga Gawel, Ewa Gibula-Bruzda, Marcin Dziedzic, Malgorzata Jenda-Wojtanowska, Marta Marszalek-Grabska, Jerzy Silberring, Jolanta H Kotlinska
Current studies indicate that the cholinergic and opioid systems interact to modulate pain. In the present work, we investigated the influence of the cholinesterase inhibitors, donepezil (0.5; 1 or 3mg/kg, i.p.) and rivastigmine (0.03; 0.5 or 1mg/kg, i.p.), on the acute antinociceptive effects of morphine (5mg/kg, i.p.) in the hot plate test in mice. Herein, both inhibitors were found to enhance and prolong the analgesic effects of morphine without affecting latencies themselves. In an extension of this work, we determined which cholinergic receptors subtype mediates the enhancement of analgesic effects of morphine, following inhibition of cholinesterases...
November 16, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27863748/ethyl-nitrobenzoate-a-novel-scaffold-for-cholinesterase-inhibition
#16
Keng Yoon Yeong, Wai-Lam Liew, Vikneswaran Murugaiyah, Chee Wei Ang, Hasnah Osman, Soo Choon Tan
A series of novel cholinesterase inhibitors containing nitrobenzoate core structure were synthesized by a facile and efficient method. The structure of the novel compounds were fully characterized and confirmed by analytical as well as spectroscopic methods. Compound indicated as 2f was found to possess the best cholinesterase inhibitory activities of all the evaluated compounds. Results suggest that 2f is a selective acetylcholinesterase inhibitor, although it also inhibits butyrylcholinesterase at higher concentration...
November 11, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27863370/novel-tacrine-1-2-3-triazole-hybrids-in%C3%A2-vitro-in%C3%A2-vivo-biological-evaluation-and-docking-study-of-cholinesterase-inhibitors
#17
Zahra Najafi, Mohammad Mahdavi, Mina Saeedi, Elahe Karimpour-Razkenari, Raymond Asatouri, Fahimeh Vafadarnejad, Farshad Homayouni Moghadam, Mahnaz Khanavi, Mohammad Sharifzadeh, Tahmineh Akbarzadeh
A new series of tacrine-1,2,3-triazole hybrids were designed, synthesized, and evaluated as potent dual cholinesterase inhibitors. Most of synthesized compounds showed good in vitro inhibitory activities toward both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Among them, 7-chloro-N-((1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl)methyl)-1,2,3,4-tetrahydroacridin-9-amine (5l) was found to be the most potent anti-AChE derivative (IC50 = 0.521 μM) and N-((1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl)methyl)-1,2,3,4-tetrahydroacridin-9-amine (5j) demonstrated the best anti-BChE activity (IC50 = 0...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27863021/synthesis-and-anti-cholinesterase-activity-of-new-substituted-benzo-d-oxazole-based-derivatives
#18
Behjat Pouramiri, Setareh Moghimi, Mohammad Mahdavi, Hamid Nadri, Alireza Moradi, Esmat Tavakolinejad-Kermani, Loghman Firoozpour, Ali Asadipour, Alireza Foroumadi
A series of novel benzo[d]oxazole derivatives (6a-n) have been synthesized and biologically evaluated as potential inhibitors of acetylcholinesterases (AChE) and butyrylcholinesterase (BChE). The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro studies showed that most of the synthesized compounds are potent acetylcholinesterase and butyrylcholinesterase inhibitors. Among them, compounds 6a and 6j strongly inhibited AChE and BChE activities with IC50 values of 1.03-1...
November 8, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27858711/cholinesterase-inhibitor-therapy-in-alzheimer-s-disease-the-limits-and-tolerability-of-irreversible-cns-selective-acetylcholinesterase-inhibition-in-primates
#19
Donald E Moss, Ruth G Perez, Haruo Kobayashi
Irreversible acetylcholinesterase (AChE) inhibition accumulates to high levels in the central nervous system (CNS) because AChE turnover in the brain is much slower than in peripheral tissues. As expected from this CNS selectivity, the irreversible AChE inhibitor methanesulfonyl fluoride (MSF) produces significant cognitive improvement in Alzheimer's disease patients without the gastrointestinal toxicity that plagues other AChE inhibitors. However, without dose-limiting gastrointestinal toxicity, one shortcoming of the prior human studies of MSF is that the upper limits of CNS AChE inhibition that might be tolerated could not be tested...
November 14, 2016: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/27856236/design-synthesis-biological-evaluation-and-molecular-modeling-studies-of-chalcone-rivastigmine-hybrids-as-cholinesterase-inhibitors
#20
Ling Wang, Yu Wang, Yiguang Tian, Jinling Shang, Xiaoou Sun, Hongzhuan Chen, Hao Wang, Wen Tan
A series of novel chalcone-rivastigmine hybrids were designed, synthesized, and tested in vitro for their ability to inhibit human acetylcholinesterase and butyrylcholinesterase. Most of the target compounds showed hBChE selective activity in the micro- and submicromolar ranges. The most potent compound 3 exhibited comparable IC50 to the commercially available drug (rivastigmine). To better understand their structure activity relationships (SAR) and mechanisms of enzyme-inhibitor interactions, kinetic and molecular modeling studies including molecular docking and molecular dynamics (MD) simulations were carried out...
November 5, 2016: Bioorganic & Medicinal Chemistry
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