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https://www.readbyqxmd.com/read/29165092/synthesis-characterization-and-biological-activities-of-new-symmetric-bis-1-2-3-triazoles-with-click-chemistry
#1
Fatih Celik, Yasemin Unver, Burak Barut, Arzu Ozel, Kemal Sancak
BACKGROUND: 1,2,3-Triazole and its derivatives have important biological activities such as antimicrobial, anti-allergic, analgesic, anti-HIV, antiinflammatory, anticancer, antimalarial and antituberculosis. Other significant triazole derivatives are 1,2,4-triazoles which play a very important role in the medicinal chemistry due to the antiinflammatory, antimicrobial, antimigraine, anticancer, antimicrobial and antimycotic activities. In this study, we aimed to synthesize a new series of bis-1,2,3-triazole derivatives including 1,2,4-triazole to obtain more effective biological activities METHODS: In this study, a new series of bis-1,2,3-triazole compounds (9,10,11) were synthesized...
November 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/29143695/an-overview-of-systematic-reviews-of-pharmacological-and-non-pharmacological-interventions-for-the-treatment-of-behavioral-and-psychological-symptoms-of-dementia
#2
Suzanne M Dyer, Stephanie L Harrison, Kate Laver, Craig Whitehead, Maria Crotty
BACKGROUND: This systematic overview reports findings from systematic reviews of randomized controlled trials of pharmacological and non-pharmacological interventions for behavioural and psychological symptoms of dementia (BPSD). METHODS: The Cochrane Database of Systematic Reviews, DARE, Medline, EMBASE, and PsycINFO were searched to September 2015. RESULTS: Fifteen systematic reviews of eighteen different interventions were included. A significant improvement in BPSD was seen with: functional analysis-based interventions (GRADE quality of evidence moderate; standardized mean difference (SMD) -0...
November 16, 2017: International Psychogeriatrics
https://www.readbyqxmd.com/read/29131306/comparative-effectiveness-and-safety-of-cognitive-enhancers-for-treating-alzheimer-s-disease-systematic-review-and-network-metaanalysis
#3
Andrea C Tricco, Huda M Ashoor, Charlene Soobiah, Patricia Rios, Areti Angeliki Veroniki, Jemila S Hamid, John D Ivory, Paul A Khan, Fatemeh Yazdi, Marco Ghassemi, Erik Blondal, Joanne M Ho, Carmen H Ng, Brenda Hemmelgarn, Sumit R Majumdar, Laure Perrier, Sharon E Straus
BACKGROUND/OBJECTIVES: To examine the comparative effectiveness and safety of cognitive enhancers for Alzheimer's disease (AD). DESIGN: Systematic review and Bayesian network metaanalysis (NMA). SETTING: MEDLINE, EMBASE, Cochrane Library, CINAHL, Ageline (inception-March 2016). PARTICIPANTS: Individuals with AD in randomized controlled trials (RCTs), quasi-RCTs, and nonrandomized studies. INTERVENTION: Any combination of donepezil, rivastigmine, galantamine, or memantine...
September 29, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/29130805/rehabilitative-success-after-brain-trauma-by-augmenting-a-subtherapeutic-dose-of-environmental-enrichment-with-galantamine
#4
Patricia B de la Tremblaye, Jody L Wellcome, Benjamin Wells de Witt, Jeffrey P Cheng, Elizabeth R Skidmore, Corina O Bondi, Anthony E Kline
BACKGROUND: Environmental enrichment (EE) confers benefits after traumatic brain injury (TBI) when provided daily for > 6 hours, but not 2 or 4 hours, which more accurately reflects the daily amount of clinical rehabilitation. The lack of benefit with sub-therapeutic EE suggests that augmentation with galantamine (GAL), which enhances cognition after TBI, may be indicated to confer benefits. OBJECTIVE: To test the hypothesis that 2 and 4 hours of EE paired with GAL will provide benefits comparable to 24 hours of EE alone...
November 1, 2017: Neurorehabilitation and Neural Repair
https://www.readbyqxmd.com/read/29126732/2-arylbenzofurans-from-artocarpus-lakoocha-and-methyl-ether-analogs-with-potent-cholinesterase-inhibitory-activity
#5
Umalee Namdaung, Anan Athipornchai, Thongchai Khammee, Mayuso Kuno, Sunit Suksamrarn
In vitro screening for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the Artocarpus lakoocha root-bark extracts revealed interesting results. Bioassay-guided fractionation resulted in the isolation of two new (1 and 2) and six known 2-arylbenzofurans 3-8, along with one stilbenoid 9 and one flavonoid 10. The structures of the isolated compounds were elucidated by UV, IR, 1D- and 2D-NMR and MS spectroscopic data analysis. Compounds 4, 6 and 7 exhibited more potent AChE inhibitory activity (IC50 = 0...
October 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29088998/post-injury-administration-of-galantamine-reduces-traumatic-brain-injury-pathology-and-improves-outcome
#6
Jing Zhao, Michael J Hylin, Nobuhide Kobori, Kimberly N Hood, Anthony N Moore, Pramod K Dash
Acetylcholine is an excitatory neurotransmitter in the central nervous system that plays a key role in cognitive function, including learning and memory. Previous studies have shown that experimental traumatic brain injury (TBI) reduces cholinergic neurotransmission, decreases evoked release of acetylcholine, and alters cholinergic receptor levels. Galantamine (FDA-approved for the treatment of vascular dementia and Alzheimer's disease) has been shown to inhibit acetylcholinesterase activity, and allosterically potentiate nicotinic receptor signaling...
October 31, 2017: Journal of Neurotrauma
https://www.readbyqxmd.com/read/29074413/galantamine-attenuates-n-n-dimethyl-hydrazine-induced-neoplastic-colon-damage-by-inhibiting-acetylcholinesterase-and-bimodal-regulation-of-nicotinic-cholinergic-neurotransmission
#7
Shreesh Raj Sammi, Jitendra K Rawat, Neetu Raghav, Ajay Kumar, Subhadeep Roy, Manjari Singh, Swetlana Gautam, Rajnish K Yadav, Uma Devi, Rakesh Pandey, Gaurav Kaithwas
The present study reveals the effect of galantamine (GAL) against 1, 2-dimethylhydrazine (DMH) induced colon cancer. Wistar albino rats were arbitrarily divided into four groups (n = 8). Group 1 served as normal control (normal saline, 3ml/kg/day, p.o.); group 2, 3 and 4 received DMH (20mg/kg/week, s.c.), for 6 weeks; groups 3 and 4 also received GAL (2 and 4mg/kg/day, p.o) for 6 weeks. DMH treated rats showed decreased heart rate variability (HRV) factors, increased incidence of aberrant crypt foci (ACF), increased thiobarbituric acid reactive substances (TBARs) along with the decrease in the enzymatic activity of superoxide dismutase (SOD) and catalase...
October 23, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28974110/acetylcholinesterase-inhibitors-beneficial-effects-on-comorbidities-in-patients-with-alzheimer-s-disease
#8
Vinod Kaushik, Sarah Toombs Smith, Emmanuel Mikobi, Mukaila A Raji
Elderly patients with Alzheimer's disease (AD) and other dementias are at high risk of polypharmacy and excessive polypharmacy for common coexisting medical conditions. Polypharmacy increases the risk of drug-drug and drug-disease interactions in these patients who may not be able to communicate early symptoms of adverse drug events. Three acetylcholinesterase inhibitors (ACHEIs) have been approved for AD: donepezil (Aricept), rivastigmine (Exelon), and galantamine (Razadyne). They are also used off-label for other causes of dementia such as Lewy body and vascular dementia...
January 1, 2017: American Journal of Alzheimer's Disease and Other Dementias
https://www.readbyqxmd.com/read/28966636/heterocyclic-compounds-as-key-structures-for-the-interaction-with-old-and-new-targets-in-alzheimer-s-disease-therapy
#9
REVIEW
Asha Hiremathad, Luca Piemontese
Nowadays, Alzheimer's disease (AD) is widely recognized as a real social problem. In fact, only five drugs are FDA approved for the therapy of this widespread neurodegenerative disease, but with low results so far. Three of them (rivastigmine, donepezil and galantamine) are acetylcholinesterase inhibitors, memantine is a N-methyl-D-aspartate receptor antagonist, whereas the fifth formulation is a combination of donepezil with memantine. The prevention and treatment of AD is the new challenge for pharmaceutical industry, as well as for public institutions, physicians, patients, and their families...
August 2017: Neural Regeneration Research
https://www.readbyqxmd.com/read/28929435/neuroprotective-effects-of-galantamine-on-nerve-agent-induced-neuroglial-and-biochemical-changes
#10
RamaRao Golime, Meehir Palit, J Acharya, D K Dubey
Neuroprotection from nerve agent such as soman-induced neural damage is a major challenge for existing drugs. Nerve agent exposure can cause many neural effects in survivors arising mainly due to acetylcholinesterase (AChE) inhibition or death within minutes. Unraveling the mechanisms underlying the nerve agent-induced multiple neurological effects is useful to develop better and safe drugs. The present study aimed to understand the molecular response during soman exposure and to evaluate the neuroprotective efficacy of galantamine on nerve agent-induced neurotoxic changes...
September 19, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28901528/beyond-symptomatic-effects-donepezil-s-potential-for-neuroprotection-and-disease-modification-in-alzheimer-s-disease
#11
REVIEW
Seung Hyun Kim, Nagaendran Kandiah, Jung-Lung Hsu, Chuthamanee Suthisisang, Chesda Udommongkol, Amitabh Dash
Alzheimer's disease (AD) is associated with neurodegenerative changes resulting clinically in progressive cognitive and functional deficits. The only therapies are the cholinesterase inhibitors (ChEIs) donepezil, galantamine, and rivastigmine and the N-methyl-D-aspartate-receptor antagonist memantine. Donepezil acts primarily on the cholinergic system as symptomatic treatment, but it also has potential for disease modification and may reduce the rate of progression of AD. This review explores the potential for a disease modifying effect of donepezil...
September 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28894228/ascorbic-acid-tethered-polymeric-nanoparticles-enable-efficient-brain-delivery-of-galantamine-an-in-vitro-in-vivo-study
#12
Kavita R Gajbhiye, Virendra Gajbhiye, Imtiaz A Siddiqui, Srikanth Pilla, Vandana Soni
The aim of this work was to enhance the transportation of the galantamine to the brain via ascorbic acid grafted PLGA-b-PEG nanoparticles (NPs) using SVCT2 transporters of choroid plexus. PLGA-b-PEG copolymer was synthesized and characterized by (1)H NMR, gel permeation chromatography, and differential scanning calorimetry. PLGA-b-PEG-NH2 and PLGA-b-mPEG NPs were prepared by nanoprecipitation method. PLGA-b-PEG NPs with desirable size, polydispersity, and drug loading were used for the conjugation with ascorbic acid (PLGA-b-PEG-Asc) to facilitate SVCT2 mediated transportation of the same into the brain...
September 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28855009/ache-inhibitors-and-nmda-receptor-antagonists-in-advanced-alzheimer-s-disease
#13
REVIEW
Brianna E Glynn-Servedio, Trisha Seys Ranola
OBJECTIVE: The objective of this article is to review the available evidence for duration of treatment with, and considerations for discontinuation of, acetylcholinesterase inhibitors and N-methyl-<small>d</small>-aspartate receptor antagonists in Alzheimer's disease. DATA SOURCES: Literature searches of clinical trials and meta-analyses were conducted using PubMed with the search terms Alzheimer's, dementia, donepezil, galantamine, memantine, and rivastigmine...
September 1, 2017: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
https://www.readbyqxmd.com/read/28837785/canagliflozin-prevents-scopolamine-induced-memory-impairment-in-rats-comparison-with-galantamine-hydrobromide-action
#14
COMPARATIVE STUDY
Nadia M S Arafa, Elham H A Ali, Mohamed Kamel Hassan
Canagliflozin (CAN) is a sodium-glucose co-transporter 2 (SGLT2) inhibitor indicated to improve glycemic control in adults with type 2 diabetes mellitus. There is a little information about its effect on the cholinergic system that proposed mechanism for memory improvement occurring by SGLT2 drugs. This study aimed to estimate the effect of CAN as compared to galantamine (GAL) treatments for two weeks on scopolamine hydrobromide (SCO)-induced memory dysfunction in experimental rats. Animals divided into six groups; control (CON), CAN, GAL, SCO, SCO + CAN and SCO + GAL...
November 1, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28832937/systematic-review-of-sex-specific-reporting-of-data-cholinesterase-inhibitor-example
#15
REVIEW
Nishila Mehta, Craig Rodrigues, Manpreet Lamba, Wei Wu, Susan E Bronskill, Nathan Herrmann, Sudeep S Gill, An-Wen Chan, Robin Mason, Suzanne Day, Jerry H Gurwitz, Paula A Rochon
OBJECTIVES: To improve the value of research for older adults, we examine sex-specific reporting of data from drug trials for the management of dementia. These data are important because they may influence considerations ranging from the health of populations to shared decision-making by individual patient and caregiver about the risk and benefit of a drug therapy. METHODS: Randomized controlled trials of cholinesterase inhibitors (i.e., donepezil, rivastigmine, or galantamine) with clinical outcomes were identified from searches of MEDLINE, EMBASE, and the Cochrane Library...
October 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/28797788/novel-dehydroabietylamine-derivatives-as-potent-inhibitors-of-acetylcholinesterase
#16
Jana Wiemann, Anne Loesche, René Csuk
Nowadays, the inhibition of acetylcholinesterase is one of the main pharmacological strategies for the treatment of Alzheimer's disease. Therefore, a set of thirty-four derivatives of the diterpenoid dehydroabietylamine has been synthesized and screened in colorimetric Ellman's assays to determine their ability to inhibit the enzymes acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine serum). A systematic variation of the substitution of dehydroabietylamides enabled an approach to analogs showing a remarkable inhibition potency for AChE...
October 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28780468/design-and-synthesis-of-2-6-di-substituted-phenyl-thiazolo-3-2-b-1-2-4-triazoles-as-%C3%AE-glucosidase-and-%C3%AE-amylase-inhibitors-co-relative-pharmacokinetics-and-3d-qsar-and-risk-analysis
#17
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Sajid Rashid, Qaiser Iqbal, Maryam Rozi, Saima Younis, Jamaluddin Mahar
Ten fused heterocyclic derivatives bearing the 2,6-di(subsituted phenyl)thiazolo[3,2-b]-1,2,4-triazoles as central rings were synthesized and structures of the compounds were established by analytical and spectral data using FTIR, EI-MS, (1)H NMR and (13)C NMR techniques. In vitro inhibitory activities of synthesized compounds on α-amylase, α-glucosidase and α-burylcholinesterase (α-BuChE) were evaluated using a purified enzyme assays. Compound 5c demonstrated strong and selective α-amylase inhibitory activity (IC50=1...
October 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28761423/galantamine-protects-against-beta-amyloid-peptide-induced-dna-damage-in-a-model-for-alzheimer-s-disease
#18
Willian O Castillo, Andres Felipe Aristizabal-Pachon
No abstract text is available yet for this article.
June 2017: Neural Regeneration Research
https://www.readbyqxmd.com/read/28760642/galantamine-administration-reduces-reactive-astrogliosis-and-upregulates-the-anti-oxidant-enzyme-catalase-in-rats-submitted-to-neonatal-hypoxia-ischemia
#19
F K Odorcyk, F Nicola, L E Duran-Carabali, F Figueiró, J Kolling, A Vizuete, E L Konrath, C A Gonçalves, A T S Wyse, C A Netto
Neonatal hypoxia ischemia (HI) plays a role in the etiology of several neurological pathologies and causes severe sequelae. Acetylcholine is a neurotransmitter in the central nervous system and cholinesterase inhibitors have demonstrated a positive action over HI induced deficits. In order to evaluate the effects of pre and post-hypoxia administrations of galantamine, a cholinesterase inhibitor, in a model of perinatal HI, Wistar rats in the post-natal day 7 (PND7) were subjected to a combination of unilateral occlusion of the right carotid artery with the exposure to a 1h hypoxia...
July 29, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28724799/galantamine-alleviates-inflammation-and-insulin-resistance-in-patients-with-metabolic-syndrome-in-a-randomized-trial
#20
Fernanda M Consolim-Colombo, Carine T Sangaleti, Fernando O Costa, Tercio L Morais, Heno F Lopes, Josiane M Motta, Maria C Irigoyen, Luiz A Bortoloto, Carlos Eduardo Rochitte, Yael Tobi Harris, Sanjaya K Satapathy, Peder S Olofsson, Meredith Akerman, Sangeeta S Chavan, Meggan MacKay, Douglas P Barnaby, Martin L Lesser, Jesse Roth, Kevin J Tracey, Valentin A Pavlov
BACKGROUND: Metabolic syndrome (MetS) is an obesity-driven condition of pandemic proportions that increases the risk of type 2 diabetes and cardiovascular disease. Pathophysiological mechanisms are poorly understood, though inflammation has been implicated in MetS pathogenesis. The aim of this study was to assess the effects of galantamine, a centrally acting acetylcholinesterase inhibitor with antiinflammatory properties, on markers of inflammation implicated in insulin resistance and cardiovascular risk, and other metabolic and cardiovascular indices in subjects with MetS...
July 20, 2017: JCI Insight
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