Article
Clinical Neurology
Alberto J. Espay, Luca Marsili, Abhimanyu Mahajan, Andrea Sturchio, Rashidkhan Pathan, Andrea Pilotto, Damodaran S. Elango, Nicole Pezous, Mario Masellis, Baltazar Gomez-Mancilla
Summary: The study evaluates the cognitive benefit of rivastigmine in patients with Parkinson's disease dementia, finding that the cognitive improvement is more significant in patients with orthostatic hypotension. Additionally, among patients with orthostatic hypotension, rivastigmine capsules showed better effects compared to patches.
ANNALS OF NEUROLOGY
(2021)
Review
Environmental Sciences
Hamed Aramjoo, Bamdad Riahi-Zanjani, Tahereh Farkhondeh, Fatemeh Forouzanfar, Mahmood Sadeghi
Summary: The specific effect of opioids on the activity of the cholinesterase enzyme is reviewed in literature, showing that opioids can induce cholinergic modulation by decreasing or increasing the enzyme activity. Different brain regions may show varying degrees of changes in ChE activity. The type of opioid used can also impact cholinergic modulation.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2021)
Article
Geriatrics & Gerontology
Nilofar Massoudi, Babak Mohit, Mohammad Fathi, Navid Nooraei, Kia Kazemzadeh Hannani, Mohsen ArianNik
Summary: This study aimed to investigate the impact of Rivastigmine as a cholinesterase inhibitor on delirium after radical surgery. The results showed that treatment with Rivastigmine was significantly associated with reduced post-operative delirium and cognitive impairment. This association became stronger after controlling for age, blood loss, and post-operative blood sodium levels. Therefore, pre-operative Rivastigmine treatment may be associated with a substantial drop in patients experiencing post-operative delirium and cognitive impairment.
INTERNATIONAL JOURNAL OF GERIATRIC PSYCHIATRY
(2023)
Article
Clinical Neurology
S. Neumann, J. Taylor, A. Bamford, C. Metcalfe, D. M. Gaunt, A. Whone, D. Steeds, S. R. Emmett, W. Hollingworth, Y. Ben-Shlomo, E. J. Henderson
Summary: This is a multi-center, double-blind, randomized placebo-controlled trial evaluating the effectiveness of a cholinesterase inhibitor on fall rate in people with idiopathic Parkinson's disease. The study aims to determine whether cholinesterase inhibitor therapy is effective in preventing falls in Parkinson's disease, and if cost-effective, it may change current management guidelines by offering a new therapeutic option for this high-risk population.
Article
Biochemistry & Molecular Biology
Minhal Yildiz, Murat Bingul, Yunus Zorlu, Mehmet F. Saglam, Mehmet Boga, Mutesir Temel, Mehmet Serdar Koca, Hakan Kandemir, Ibrahim F. Sengul
Summary: A range of novel indole based thiosemicarbazone derivatives were synthesized and studied for their potential as cholinesterase inhibitors and antioxidants. Compounds 18 and 19 showed the best inhibitory activity against butyrylcholinesterase and exhibited moderate antioxidant potential. Molecular docking studies suggested that compound 19 could compete with galantamine as a cholinesterase inhibitor.
BIOORGANIC CHEMISTRY
(2022)
Article
Medicine, General & Internal
Shanquan Chen, Annabel C. Price, Rudolf N. Cardinal, Sinead Moylett, Anne D. Kershenbaum, James Fitzgerald, Christoph Mueller, Robert Stewart, John T. O'Brien
Summary: This study aimed to investigate the association between the use of acetylcholinesterase inhibitors (AChEIs) and/or memantine in patients with dementia with Lewy bodies (DLBs) and their hospital admissions and mortality rates. The results showed that the use of AChEIs and/or memantine was associated with a reduced risk of death and shorter hospital stays for DLB patients.
Article
Psychiatry
Marieke J. Henstra, Thomas C. Feenstra, Rob M. Kok, Harm-Pieter Spaans, Eric van Exel, Annemiek Dols, Mardien Oudega, Anton C. M. Vergouwen, Adriano van der Loo, Pierre M. Bet, Stephan A. Loer, Merijn Eikelenboom, Pascal Sienaert, Simon Lambrichts, Filip Bouckaert, Judith E. Bosmans, Nathalie van der Velde, Aartjan T. F. Beekman, Max L. Stek, Didi Rhebergen
Summary: This study focuses on the inter-ictal delirium induced by ECT and aims to examine the effect of rivastigmine on this side-effect. The study combines a cohort study on older patients with depression treated with ECT with a randomized, placebo-controlled cross-over trial. It provides an opportunity to understand the cognitive side-effects of ECT and identify potential determinants.
FRONTIERS IN PSYCHIATRY
(2022)
Article
Biochemistry & Molecular Biology
Sarfaraz Shaikh, Ganesh Pavale, Pratik Dhavan, Pinky Singh, Jasmin Uparkar, S. P. Vaidya, B. L. Jadhav, M. M. Ramana
Summary: A series of novel dihydropyranoindole derivatives containing sulphonamide group were synthesized and evaluated for their in-vitro anti-cholinesterase activity. The most potent compound showed strong inhibition towards AChE and BuChE, as well as antioxidant and DNA damage protection activities, with good pharmacokinetic properties demonstrated in ADME studies. These findings suggest that dihydropyranoindole derivatives could be potential drug leads in the search for new multifunctional AD drugs.
BIOORGANIC CHEMISTRY
(2021)
Article
Medicine, General & Internal
Mahdieh Sadeghi, Zakaria Zakariaei, Mostafa Soleymani, Abdollah Malakian
Summary: This article describes a case of a 2-year-old infant who developed cholinergic syndrome after accidental ingestion of donepezil tablets and was discharged in stable condition.
CLINICAL CASE REPORTS
(2022)
Review
Neurosciences
Maja Przybylowska, Krystyna Dzierzbicka, Szymon Kowalski, Klaudia Chmielewska, Iwona Inkielewicz-Stepniak
Summary: This review examines the development of tacrine analogues and other drug hybrids in the past three years for the treatment of Alzheimer's disease, highlighting their potential multifunctional therapeutic effects and related mechanisms.
CURRENT NEUROPHARMACOLOGY
(2021)
Review
Pharmacology & Pharmacy
Shahid Yousuf Ganie, Darakhshan Javaid, Younis Ahmad Hajam, Mohd Salim Reshi
Summary: Organophosphates (OPs) are commonly used pesticides that can cause neurotoxic effects and other disorders. Humans are exposed to OPs through different routes and biomonitoring of OP markers can help measure and control exposure severity. Standard treatments for OP poisoning include administration of atropine and acetylcholine esterase restoration therapy. It is important to increase awareness about the potential risks of OP exposure and reevaluate exposure levels.
Article
Chemistry, Organic
Javed Iqbal, Ali Imran Mallhi, Aziz Ur Rehman, Samiah H. Al-Mijalli, Mehr Un-Nisa, Fatiqa Zafar, Sohail Shahzad, Shahid Rasool, Munawar Iqbal, Syed Adnan Ali Shah
Summary: N-Substituted-2-propanamide analogues of 1,3,4-oxadiazole have been synthesized and screened for their inhibition potential against enzymes. Molecular docking investigations were used to understand the structure-activity relationship of the compounds and their interaction with enzyme active sites. Further studies on pharmacodynamics, pharmacokinetics and in vivo effects are needed for the most active compounds.
HETEROCYCLIC COMMUNICATIONS
(2023)
Article
Chemistry, Medicinal
Resit Cakmak, Eyup Basaran, Murat Senturk
Summary: In this study, novel Schiff base derivatives containing a pyrazolone ring were synthesized and tested for their inhibitory activities on several enzymes. The compounds showed significant inhibition effects and may serve as potential drug candidates.
ARCHIV DER PHARMAZIE
(2022)
Article
Fisheries
Alshimaa A. Khalil, Yasmina M. Abd-Elhakim, Enas N. Said, Attia A. A. Moselhy, Abdelghafar M. Abu-Elsaoud, Walaa El-Houseiny
Summary: This study investigated the effects of milk thistle powder (MTP) and/or co-enzyme Q10 (CoQ10) supplementation on the neurobehavioral performance, brain oxidative status, and histological picture in Nile tilapia reared in nickel-polluted water. The results showed that MTP and/or CoQ10 supplementation reversed the negative effects of nickel on feeding behavior and aggression, restored antioxidant brain content, reduced malondialdehyde levels, and mitigated histopathological abnormalities. Overall, MTP and CoQ10 achieved the best neurobehavioral performance and brain oxidative status.
Article
Pharmacology & Pharmacy
Kajal Tak, Prashansa Sharma, Rekha Sharma, Vivek Dave, Smita Jain, Swapnil Sharma
Summary: This study reports the synthesis of Donepezil hydrochloride functionalized Graphene quantum dots (DO-ptGQD) for the treatment of Alzheimer's disease. The ptGQD was synthesized using a one-pot hydrothermal synthesis method with the root extract of Polygala tenuifolia. The synthesized ptGQD was evaluated using various techniques and the formulated DO-ptGQD was further evaluated for its effectiveness in in-vitro and in-vivo models. The outcomes of the study showed that DO-ptGQD improved learning and memory abilities, had a higher inhibition of AchE enzyme, increased protein and glutathione levels, and decreased nitric oxide and lipid peroxide levels. The histopathological image also indicated that DO-ptGQD treated cell disorganization and preserved small pyramidal cells better compared to other formulations. In conclusion, DO-ptGQD is a safe and effective drug delivery system for the treatment of Alzheimer's disease, and the root extract of Polygala tenuifolia provides a synergistic effect for the treatment of the disease.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Article
Chemistry, Organic
Dilek Isik Tasgin, Irem Bayraktar
Summary: We present a synthetic method for pyrrolizine-3-one derivatives and investigate their photophysical properties. These compounds are prepared through a series of reactions involving substituted pyrroles in one-pot, two-step oxidation, and intramolecular cyclization processes. The photophysical properties of the synthesized compounds are studied using UV-Vis and fluorescence spectroscopy in various solvents. The introduction of pyrrolyl substituents has a significant impact on Stokes shifts and quantum yield values.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Satish Kumar Burra, Vaikunta Rao Lakinani, Raghunadh Akula, Chiranjeevi Yankkanti
Summary: A novel and green strategy for the construction of biologically relevant substituted indolyl-4H-chromenes scaffolds is reported, using L-proline as a catalyst and water as a promoter solvent. This catalytic system offers wider applicability, shorter reaction times, and high yields, making it an ideal condition for green chemistry.
SYNTHETIC COMMUNICATIONS
(2024)
Review
Chemistry, Organic
Abouelhaoul El Alami, Amine El Maraghi, Fatima Youssoufi, Assiya Atif, Hamid Sdassi
Summary: Nitrobenzimidazoles have become increasingly important in the design of new compounds in medicinal, therapeutic and chemical fields. This review provides an overview of the synthesis strategies and biological activities of nitrobenzimidazole derivatives.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Nilesh Raghunath Khedkar, Alex Joseph, Milind Sindkhedkar
Summary: In this study, a new library of 3-(2-(pyrimidin-5-yl)thiazol-4-yl)-1,2,4-oxadiazole compounds was designed and synthesized as potential anticancer agents using in silico fragment-based drug design. The compounds were tested for their anticancer activity in vitro, and one compound exhibited excellent activity against multiple cancer cell lines.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Terungwa H. Iorkula, Bryce A. Tolman, Scott R. Burt, Matt A. Peterson
Summary: A new method for synthesizing C-6 substituted products has been discovered in this study, which utilizes lower doses of fluoride and CsF as a catalyst, with high reaction yields and cost-effectiveness under suitable conditions.
SYNTHETIC COMMUNICATIONS
(2024)
Review
Chemistry, Organic
Ranjana Aggarwal, Swati Sharma
Summary: This review article mainly focuses on the synthesis of 3(5)-trifluoromethylpyrazoles via condensation reaction of trifluoromethyl-beta-diketones with hydrazines. It emphasizes the importance of fluorine-containing compounds and pyrazoles in the field of biology. The literature reported condensation reactions of trifluoromethyl-beta-diketones with hydrazines are covered.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
F. M. Alshareef, Sami A. Al-Harbi, Esam S. Allehyani, Omeima Abdullah, Magdy A. Ibrahim
Summary: This study aimed to construct a novel category of linear annulated chromeno[3',2':5,6]pyrido[2,3-d][1,3]thiazolo[3,2-a]pyrimidines. The chemical reactivity of the synthesized compounds was investigated, and they showed significant antimicrobial activity against various strains.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Preethi Dhanapal, S. L. Manju
Summary: Thiazole based Schiff base scaffolds have become an integral part of drug development in recent years, playing a versatile role as building blocks for lead drug molecules. This study presents a facile one pot synthetic method for producing novel 4-aryl thiazoles with high yield, shorter reaction time, and milder conditions, without the need for catalysts or purification techniques.
SYNTHETIC COMMUNICATIONS
(2024)