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https://www.readbyqxmd.com/read/27914796/design-and-synthesis-of-new-piperidone-grafted-acetylcholinesterase-inhibitors
#1
Alireza Basiri, Michelle Xiao, Alec McCarthy, Debashis Dutta, Siddappa N Byrareddy, Martin Conda-Sheridan
Alzheimer's disease (AD) is a neurodegenerative disorder affecting 35million people worldwide. A common strategy to improve the well-being of AD patients consists on the inhibition of acetylcholinesterase with the concomitant increase of the neurotransmitter acetylcholine at cholinergic synapses. Two series of unreported N-benzylpiperidines 5(a-h) and thiazolopyrimidines 9(a-q) molecules were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) inhibitory activities. Among the newly synthesized compounds, 5h, 9h, 9j, and 9p displayed higher AChE enzyme inhibitory activities than the standard drug, galantamine, with IC50 values of 0...
November 24, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27900576/time-course-behavioral-safety-and-protective-efficacy-of-centrally-active-reversible-acetylcholinesterase-inhibitors-in-cynomolgus-macaques
#2
Lindsey R Hamilton, Steven C Schachter, Todd M Myers
Galantamine hydrobromide and (-)huperzine A, centrally active reversible acetylcholinesterase inhibitors, are potentially superior to the current standard, pyridostigmine bromide, as a pretreatment for organophosphorus chemical warfare nerve agent intoxication. Galantamine, huperzine, and pyridostigmine were compared for time course of acetylcholinesterase inhibition in 12 cynomolgus macaques. Although both galantamine and huperzine shared a similar time course profile for acetylcholinesterase inhibition, huperzine was 88 times more potent than galantamine...
November 30, 2016: Neurochemical Research
https://www.readbyqxmd.com/read/27896785/prescription-patterns-of-medications-for-alzheimer-s-disease-in-japan-from-2010-to-2015-a-descriptive-pharmacy-claims-database-study
#3
Kimiko Kadohara, Izumi Sato, Yuko Doi, Masaru Arai, Yosuke Fujii, Toshiyuki Matsunaga, Koji Kawakami
INTRODUCTION: Although four kinds of Alzheimer's disease (AD) drugs are available at present there was only one drug until 2011 in Japan. This study aimed to elucidate prescription trends of these medications for AD in Japanese outpatients before and after the new drug releases in 2011. METHODS: This descriptive study of pharmacy claims databases analyzed outpatient prescription data from community pharmacies across Japan. The study patients were 20 years or older and first administered medications for AD (donepezil, memantine, rivastigmine, or galantamine) between January 2010 and September 2014...
November 28, 2016: Neurology and Therapy
https://www.readbyqxmd.com/read/27876467/a-review-on-tacrine-based-scaffolds-as-multi-target-drugs-mtdls-for-alzheimer-s-disease
#4
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/27846868/effect-of-concomitant-use-of-memantine-on-mortality-and-efficacy-outcomes-of-galantamine-treated-patients-with-alzheimer-s-disease-post-hoc-analysis-of-a-randomized-placebo-controlled-study
#5
Klaus Hager, Alan S Baseman, Jeffrey S Nye, H Robert Brashear, John Han, Mary Sano, Bonnie Davis, Henry M Richards
BACKGROUND: A large, prospective, 2-year, randomized study in patients with mild-to-moderate Alzheimer's disease or mixed dementia demonstrated reductions in mortality and cognitive/functional decline in galantamine-treated patients. A post-hoc analysis was conducted to study the effect of (the presence or absence of) concomitant memantine use on treatment outcome. METHODS: Randomized patients (N = 2045) were divided into subgroups based on memantine use. Analyses included demographic and clinical characteristics (age, nursing home placement, Mini-Mental State Examination (MMSE) and Disability Assessment for Dementia (DAD) scores) and mortality endpoints...
November 15, 2016: Alzheimer's Research & Therapy
https://www.readbyqxmd.com/read/27829466/dendropanax-morbifera-l%C3%A3-veille-extract-ameliorates-cadmium-induced-impairment-in-memory-and-hippocampal-neurogenesis-in-rats
#6
Woosuk Kim, Hee Sun Yim, Dae Young Yoo, Hyo Young Jung, Jong Whi Kim, Jung Hoon Choi, Yeo Sung Yoon, Dae Won Kim, In Koo Hwang
BACKGROUND: Cadmium leads to learning and memory impairment. Dendropanax morbifera Léveille stem extract (DMS) reduces cadmium-induced oxidative stress in the hippocampus. We investigated the effects of DMS on cadmium-induced impairments in memory in rats. METHODS: Cadmium (2 mg/kg), with or without DMS (100 mg/kg), was orally administered to 7-week-old Sprague-Dawley rats for 28 days. Galantamine (5 mg/kg), an acetylcholinesterase inhibitor, was intraperitoneally administered as a positive control...
November 9, 2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27806662/galantamine-and-environmental-enrichment-enhance-cognitive-recovery-after-experimental-traumatic-brain-injury-but-do-not-confer-additional-benefits-when-combined
#7
Patricia B de la Tremblaye, Corina O Bondi, Naima Lajud, Jeffrey P Cheng, Hannah Radabaugh, Anthony E Kline
Environmental enrichment (EE) enhances cognition after traumatic brain injury (TBI). Galantamine (GAL) is an acetylcholinesterase inhibitor that may also promote benefits. Hence, the aims of this study were to assess the efficacy of GAL alone (standard (STD) housing) and in combination with EE in adult male rats after TBI. The hypothesis was that both therapies would confer motor, cognitive, and histological benefits when provided singly, but their combination would be more efficacious. Anesthetized rats received a controlled cortical impact or sham injury and then were randomly assigned to receive GAL (1, 2, or 3 mg/kg; i...
November 2, 2016: Journal of Neurotrauma
https://www.readbyqxmd.com/read/27786552/use-of-antidementia-drugs-and-risk-of-pneumonia-in-older-persons-with-alzheimer-s-disease
#8
Pasi Lampela, Anna-Maija Tolppanen, Antti Tanskanen, Jari Tiihonen, Piia Lavikainen, Sirpa Hartikainen, Heidi Taipale
INTRODUCTION: Persons with Alzheimer's disease are at an increased risk of pneumonia, but the comparative risks during specific antidementia treatments are not known. We compared the risk of pneumonia in use of donepezil, rivastigmine (oral, transdermal), galantamine and memantine. PATIENTS AND METHODS: We used data from a nationwide cohort of community-dwelling individuals diagnosed with Alzheimer's disease during 2005-2011 in Finland, who initiated monotherapy with acetylcholinesterase inhibitor or memantine (n = 65481)...
October 27, 2016: Annals of Medicine
https://www.readbyqxmd.com/read/27773692/pretreatment-and-prophylaxis-against-nerve-agent-poisoning-are-undesirable-behavioral-side-effects-unavoidable
#9
REVIEW
Trond Myhrer, Pål Aas
The threat of chemical warfare agents like nerve agents requires life saving measures of medical pretreatment combined with treatment after exposure. Pretreatment (pyridostigmine) may cause some side effects in a small number of individuals. A comprehensive research on animals has been performed to clarify effects on behavior. The results from these studies are far from unambiguous, since pyridostigmine may produce adverse effects on behavior in animals in relatively high doses, but not in a consistent way...
December 2016: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/27689726/repurposing-n-n-bis-arylamidino-1-4-piperazinedicarboxamidines-an-unexpected-class-of-potent-inhibitors-of-cholinesterases
#10
Anne Loesche, Jana Wiese, Sven Sommerwerk, Vivienne Simon, Wolfgang Brandt, René Csuk
Drug repurposing (=drug repositioning) is an effective way to cut costs for the development of new therapeutics and to reduce the time-to-market time-span. Following this concept a small library of compounds was screened for their ability to act as inhibitors of acetyl- and butyrylcholinesterase. Picloxydine, an established antiseptic, was shown to be an inhibitor for both enzymes. Systematic variation of the aryl substituents led to analogs possessing almost the same good properties as gold standard galantamine hydrobromide...
September 19, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27681239/synthesis-and-evaluation-of-dihydropyrimidinone-derived-selenoesters-as-multi-targeted-directed-compounds-against-alzheimer-s-disease
#11
Flavio A R Barbosa, Rômulo F S Canto, Sumbal Saba, Jamal Rafique, Antonio L Braga
This paper describes the synthesis and evaluation of new dihydropyrimidinone (DHPM)-derived selenoesters as potential multi-targeted agents for the treatment of Alzheimer's disease. A series of DHPM-derived selenoesters were obtained with high structural diversity through a short and modular synthetic route. The antioxidant activity was evaluated by TBARS and iron chelation assays. These compounds were also evaluated as acetylcholinesterase inhibitors (AChEi). The compounds demonstrated good antioxidant activity, since they presented excellent lipid peroxidation inhibition and good iron chelation activity...
September 13, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27660276/in-vitro-effects-of-cognitives-and-nootropics-on-mitochondrial-respiration-and-monoamine-oxidase-activity
#12
Namrata Singh, Jana Hroudová, Zdeněk Fišar
Impairment of mitochondrial metabolism, particularly the electron transport chain (ETC), as well as increased oxidative stress might play a significant role in pathogenesis of Alzheimer's disease (AD). Some effects of drugs used for symptomatic AD treatment may be related to their direct action on mitochondrial function. In vitro effects of pharmacologically different cognitives (galantamine, donepezil, rivastigmine, 7-MEOTA, memantine) and nootropic drugs (latrepirdine, piracetam) were investigated on selected mitochondrial parameters: activities of ETC complexes I, II + III, and IV, citrate synthase, monoamine oxidase (MAO), oxygen consumption rate, and hydrogen peroxide production of pig brain mitochondria...
September 23, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27622387/time-related-effects-on-functional-brain-connectivity-after-serotonergic-and-cholinergic-neuromodulation
#13
Bernadet L Klaassens, Serge A R B Rombouts, Anderson M Winkler, Helene C van Gorsel, Jeroen van der Grond, Joop M A van Gerven
Psychopharmacological research, if properly designed, may offer insight into both timing and area of effect, increasing our understanding of the brain's neurotransmitter systems. For that purpose, the acute influence of the selective serotonin reuptake inhibitor citalopram (30 mg) and the acetylcholinesterase inhibitor galantamine (8 mg) was repeatedly measured in 12 healthy young volunteers with resting state functional magnetic resonance imaging (RS-fMRI). Eighteen RS-fMRI scans were acquired per subject during this randomized, double blind, placebo-controlled, crossover study...
September 13, 2016: Human Brain Mapping
https://www.readbyqxmd.com/read/27618041/color-change-of-phenol-red-by-integrated-smart-phone-camera-as-a-tool-for-the-determination-of-neurotoxic-compounds
#14
Adam Kostelnik, Alexander Cegan, Miroslav Pohanka
The use of a cell phone as a detection system is easy, simple and does not require trained personnel, which is in contrast to standard laboratory instruments. This paper deals with immobilization of acetylcholinesterase (AChE) in a gelatin matrix, and phenol red, as an indicator of AChE activity, is used in order to establish a method that is easily compatible with a camera device. AChE splits acetylcholine into choline and acetic acid, which changes the pH of a medium, resulting in a phenol red color change...
September 7, 2016: Sensors
https://www.readbyqxmd.com/read/27609215/in-vivo-characterization-of-arn14140-a-memantine-galantamine-based-multi-target-compound-for-alzheimer-s-disease
#15
Angelo M Reggiani, Elena Simoni, Roberta Caporaso, Johann Meunier, Emeline Keller, Tangui Maurice, Anna Minarini, Michela Rosini, Andrea Cavalli
Alzheimer's disease (AD) is a chronic pathological condition that leads to neurodegeneration, loss of intellectual abilities, including cognition and memory, and ultimately to death. It is widely recognized that AD is a multifactorial disease, where different pathological cascades (mainly amyloid and tau) contribute to neural death and to the clinical outcome related to the disease. The currently available drugs for AD were developed according to the one-target, one-drug paradigm. In recent times, multi-target strategies have begun to play an increasingly central role in the discovery of more efficacious candidates for complex neurological conditions, including AD...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27592396/new-piperidine-hydrazone-derivatives-synthesis-biological-evaluations-and-molecular-docking-studies-as-ache-and-bche-inhibitors
#16
Nurcan Karaman, Yusuf Sıcak, Tuğba Taşkın-Tok, Mehmet Öztürk, Ayşegül Karaküçük-İyidoğan, Miris Dikmen, Bedia Koçyiğit-Kaymakçıoğlu, Emine Elçin Oruç-Emre
Hydrazones and the piperidine ring containing compounds were considered as beneficial substrates in drug design. Therefore, this study was aimed at the synthesis of new benzoyl hydrazones derived from ethyl 4-oxopiperidine-1-carboxylate and 2,6-diphenylpiperidin-4-one. The synthesized compounds (1-19) were screened for their antioxidant, anticholinesterase and anticancer activities. The antioxidant capacity of the compounds was evaluated by using four complementary tests. The results showed that compound 7 and 17 have the higher lipid peroxidation inhibitory activity than the other compounds...
August 20, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27589716/extracts-from-traditional-chinese-medicinal-plants-inhibit-acetylcholinesterase-a-known-alzheimer-s-disease-target
#17
Dorothea Kaufmann, Anudeep Kaur Dogra, Ahmad Tahrani, Florian Herrmann, Michael Wink
Inhibition of acetylcholinesterase (AChE) is a common treatment for early stages of the most general form of dementia, Alzheimer's Disease (AD). In this study, methanol, dichloromethane and aqueous crude extracts from 80 Traditional Chinese Medical (TCM) plants were tested for their in vitro anti-acetylcholinesterase activity based on Ellman's colorimetric assay. All three extracts of Berberis bealei (formerly Mahonia bealei), Coptis chinensis and Phellodendron chinense, which contain numerous isoquinoline alkaloids, substantially inhibited AChE...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27582416/effect-of-mesenchymal-stem-cells-and-galantamine-nanoparticles-in-rat-model-of-alzheimer-s-disease
#18
Shubham Misra, Kanwaljit Chopra, Uma Nahar Saikia, Vivek Ranjan Sinha, Rakesh Sehgal, Manish Modi, Bikash Medhi
AIM: The present study investigated the efficacy of bone marrow-derived mesenchymal stem cells (BM-MSCs) in combination with galantamine hydrobromide-loaded solid lipid nanoparticles (GH-SLNs) in intracerebroventricular (ICV)-isoproterenol-induced rat model of Alzheimer's disease. MATERIALS & METHODS: BM-MSCs were harvested by dissecting femur and tibia of 8-10-week-old Wistar rats. 1 × 10(6) cells were administered intravenously once in ICV-isoproterenol-induced rats followed by GH-SLNs (5 mg/kg) for 3 weeks...
October 2016: Regenerative Medicine
https://www.readbyqxmd.com/read/27581632/synthesis-biological-evaluation-and-molecular-docking-study-of-hydrazone-containing-pyridinium-salts-as-cholinesterase-inhibitors
#19
Sulunay Parlar, Gulsah Bayraktar, Ayse Hande Tarikogullari, Vildan Alptüzün, Ercin Erciyas
A series of pyridinium salts bearing alkylphenyl groups at 1 position and hydrazone structure at 4 position of the pyridinium ring were synthesized and evaluated for the inhibition of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) enzymes. The cholinesterase (ChE) inhibitory activity studies were carried out by using the Ellman's colorimetric method. All compounds displayed considerable AChE and BuChE inhibitory activity and some of the compounds manifested remarkable anti-AChE activity compared to the reference compound, galantamine...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27578455/comprehensive-effects-of-galantamine-and-cilostazol-combination-therapy-on-patients-with-alzheimer-s-disease-with-asymptomatic-lacunar-infarction
#20
Nozomi Hishikawa, Yusuke Fukui, Kota Sato, Yasuyuki Ohta, Toru Yamashita, Koji Abe
AIM: The coexistence of Alzheimer's disease (AD) and cerebrovascular disease pathology increases age-dependently. We comprehensively analyzed the clinical effects of galantamine or cilostazol monotherapy to the add-on combination therapy on three major factors of dementia, such as cognitive, affective and activities of daily living functions in AD patients with asymptomatic lacunar infarction. METHODS: We divided 101 AD patients with asymptomatic lacunar infarction into two subgroups: group A (n = 61, first treated with galantamine and then cilostazol added) and group B (n = 40, first treated with cilostazol and galantamine added)...
August 31, 2016: Geriatrics & Gerontology International
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