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https://www.readbyqxmd.com/read/28524136/-clinical-evaluation-of-the-effectiveness-of-cholinesterase-inhibition-with-neuromidin-in-the-treatment-of-primary-glaucoma-patients
#1
I A Zakharova, R V Avdeev, V A Pristavka, S N Surnin, V Yu Makhmutov, I I Savrasova
AIM: to investigate neuromidin effectiveness in the treatment of patients with primary glaucoma and compensated intraocular pressure (IOP). MATERIAL AND METHODS: A total of 40 patients (80 eyes) were examined. Of them, 10 eyes with early glaucoma, 36 eyes with moderate-stage glaucoma, 33 eyes with advanced glaucoma, and 1 eye with end-stage glaucoma. In 19 eyes, IOP was controlled through beta-blockers, in 11 eyes - through carbonic anhydrase inhibitors, in 10 eyes - through prostaglandin analogues, and in 39 eyes - through combination drugs...
2017: Vestnik Oftalmologii
https://www.readbyqxmd.com/read/28514891/synergistic-effect-of-rapamycin-and-metformin-against-age-dependent-oxidative-stress-in-rat-erythrocyte
#2
Abhishek Kumar Singh, Geetika Garg, Sandeep Singh, Syed Ibrahim Rizvi
Erythrocytes are particularly vulnerable towards age-dependent oxidative stress mediated damage. Caloric restriction mimetics (CRMs) may provide a novel strategy for the maintenance of redox balance as well as effective treatment of age associated diseases. Herein, we have investigated the beneficial effect of co-treatment of CRM-candidate drugs, rapamycin (an immunosuppressant drug and inhibitor of mammalian target of rapamycin) and metformin (an anti-diabetic biguanide and activator of adenosine monophosphate kinase) against aging-induced oxidative stress in erythrocytes and plasma of aging rats...
May 17, 2017: Rejuvenation Research
https://www.readbyqxmd.com/read/28511871/effect-of-distigmine-on-the-contractile-response-of-guinea-pig-urinary-bladder-to-electrical-field-stimulation
#3
Keisuke Obara, Yurina Kobayashi, Daisuke Chino, Yoshio Tanaka
Distigmine bromide (distigmine) is a reversible carbamate group cholinesterase (ChE) inhibitor. Although mainly used clinically for the treatment of myasthenia gravis, distigmine is also indicated for detrusor underactivity in Japan. According to the pharmacological classification of distigmine, its therapeutic effect against detrusor underactivity appears to be produced by enhanced urinary bladder smooth muscle (UBSM) contractility due to an increased concentration of acetylcholine between parasympathetic nerve endings and UBSM cells...
May 13, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28508250/a-real-world-analysis-of-treatment-patterns-for-cholinesterase-inhibitors-and-memantine-among-newly-diagnosed-alzheimer-s-disease-patients
#4
Nawal Bent-Ennakhil, Florence Coste, Lin Xie, Myrlene Sanon Aigbogun, Yuexi Wang, Furaha Kariburyo, Ann Hartry, Onur Baser, Peter Neumann, Howard Fillit
INTRODUCTION: Alzheimer's disease (AD) is the most common neurodegenerative form of dementia. Pharmacological therapies for symptomatic treatment, such as acetylcholinesterase inhibitors (AChEIs) and memantine, have been available in the USA since 2000. Over the past decade, few studies have analyzed real-world anti-dementia treatment patterns in the USA. This study evaluated monotherapy AChEIs and memantine treatment patterns among newly diagnosed AD patients. METHODS: A retrospective cohort study was conducted using Medicare data and the Minimum Data Set from 2008 to 2012...
May 15, 2017: Neurology and Therapy
https://www.readbyqxmd.com/read/28505534/discorhabdin-alkaloids-from-antarctic-latrunculia-spp-sponges-as-a-new-class-of-cholinesterase-inhibitors
#5
Tanja Botić, Andrea Defant, Pietro Zanini, Monika Cecilija Žužek, Robert Frangež, Dorte Janussen, Daniel Kersken, Željko Knez, Ines Mancini, Kristina Sepčić
The brominated pyrroloiminoquinone alkaloids discorhabdins B, L and G and 3-dihydro-7,8- dehydrodiscorhabdin C, isolated from methanol extracts of two specimens of Latrunculia sp. sponges collected near the Antarctic Peninsula, are here demonstrated for the first time to be reversible competitive inhibitors of cholinesterases. They showed Ki for electric eel acetylcholinesterase of 1.6-15.0 μM, for recombinant human acetylcholinesterase of 22.8-98.0 μM, and for horse serum butyrylcholinesterase of 5.0-76...
May 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28504912/synthesis-and-biological-assessment-of-racemic-benzochromenopyrimidinetriones-as-promising-agents-for-alzheimer-s-disease-therapy
#6
Youssef Dgachi, Helène Martin, Alexandre Bonet, Mourad Chioua, Isabel Iriepa, Ignacio Moraleda, Fakher Chabchoub, José Marco-Contelles, Lhassane Ismaili
AIM: Due to the complex nature of Alzheimer's disease, there is a renewed search for multitarget directed drugs. RESULTS: This paper describes the synthesis and in vitro biological evaluation of six racemic 13-aryl-2,3,4,13-tetrahydro-1H,12H-benzo[6,7]chromeno[2,3-d]pyrido[1,2-a]pyrimidine-7,12,14-triones (1a-6a), and six racemic 15-aryl-8,9,10,11,12,15-hexahydro-14H-benzo[6',7']chromeno[2',3:4,5] pyr-imido [1,2-a]azepine-5,14,16-triones (1b-6b), showing antioxidant and cholinesterase inhibitory capacity...
May 15, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28504893/dual-inhibitors-of-cholinesterases-and-monoamine-oxidases-for-alzheimer-s-disease
#7
Damijan Knez, Matej Sova, Urban Košak, Stanislav Gobec
Accumulating evidence indicates a solid relationship between several enzymes and Alzheimer's disease. Cholinesterases and monoamine oxidases are closely associated with the disease symptomatology and progression and have been tackled simultaneously using several multifunctional ligands. This design strategy offers great chances to alter the course of Alzheimer's disease, in addition to alleviation of the symptoms. More than 15 years of research has led to the identification of various dual cholinesterase/monoamine oxidase inhibitors, while some showing positive outcomes in clinical trials, thus giving rise to additional research efforts in the field...
May 15, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28501648/tetrahydroacridine-derivatives-with-fluorobenzoic-acid-moiety-as-multifunctional-agents-for-alzheimer-s-disease-treatment
#8
Kamila Czarnecka, Paweł Szymański, Małgorzata Girek, Elżbieta Mikiciuk-Olasik, Robert Skibiński, Jacek Kabziński, Ireneusz Majsterek, Barbara Malawska, Jakub Jończyk, Marek Bajda
A novel series of 9-amino-1,2,3,4-tetrahydroacridine derivatives with 2-fluorobenzoic acid or 3-fluorobenzoic acid moiety were designed, synthesized and evaluated as inhibitors of cholinesterases and aggregation of β-amyloid. In the study target compounds were very potent inhibitors of AChE and BChE. The most promising agents had higher inhibitory potency than the reference drugs which was tacrine. Ultimately, the kinetic assay shows the most active target compound 3c against AChE. Almost all of them were more potent against BChE than AChE...
May 5, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28501487/inhibition-on-cholinesterase-and-tyrosinase-by-alkaloids-and-phenolics-from-aristotelia-chilensis-leaves
#9
Carlos L Cespedes, Cristian Balbontin, Jose G Avila, Mariana Dominguez, Julio Alarcon, Cristian Paz, Viviana Burgos, Leandro Ortiz, Ignacio Peñaloza-Castro, David S Seigler, Isao Kubo
It is reported in this study the effect of isolates from leaves of Aristotelia chilensis as inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and tyrosinase enzymes. The aim of the paper was to evaluate the activity of A. chilensis towards different enzymes. In addition to pure compounds, extracts rich in alkaloids and phenolics were tested. The most active F5 inhibited AChE (79.5% and 89.8% at 10.0 and 20.0 μg/mL) and against BChE (89.5% and 97.8% at 10.0 and 20.0 μg/mL), showing a strong mixed-type inhibition against AChE and BChE...
May 10, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28498775/chalcone-based-carbamates-for-alzheimer-s-disease-treatment
#10
Angela Rampa, Serena Montanari, Letizia Pruccoli, Manuela Bartolini, Federico Falchi, Alessandra Feoli, Andrea Cavalli, Federica Belluti, Silvia Gobbi, Andrea Tarozzi, Alessandra Bisi
AIM: Alzheimer's disease is a still untreatable multifaceted pathology, and drugs able to stop or reverse its progression are urgently needed. In this picture, the recent reformulation of the cholinergic hypothesis renewed the interest for acetylcholinesterase inhibitors. In this paper, a series of naturally inspired chalcone-based carbamates was designed to target cholinesterase enzymes and possibly generate fragments endowed with neuroprotective activity in situ. Results & methodology: All compounds presented in this study showed nanomolar potency for cholinesterase inhibition...
May 12, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28497326/evaluation-of-pelvic-inflammatory-disease-potential-in-cholinesterase-inhibitor-pesticide-exposed-females
#11
Eman I Draz, Azza M Hassan, Haidy S Khalil, Mohamed A Elomary
Cholinesterase inhibitor pesticides, mainly organophosphates and carbamates, are commonly used in Egypt. Chronic exposure of males and females working in agriculture is expected. The study aimed to relate exposure to cholinesterase inhibitor pesticides to the development of pelvic inflammatory disease (PID). This is a case-control study that was conducted among 84 females. Seventy patients complained of pelvic inflammatory disease visited the outpatient Gynecology and Obstetrics Clinic. Fourteen females were not suffering from PID and were chosen as a control group...
May 11, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28495556/synthesis-crystal-structure-determination-biological-screening-and-docking-studies-of-n-1-substituted-derivatives-of-2-3-dihydroquinazolin-4-1h-one-as-inhibitors-of-cholinesterases
#12
Nargis Sultana, Muhammad Sarfraz, Saba Tahir Tanoli, Muhammad Safwan Akram, Abdul Sadiq, Umer Rashid, Muhammad Ilyas Tariq
Pursuing the strategy of developing potent AChE inhibitors, we attempted to carry out the N(1)-substitution of 2,3-dihydroquinazolin-4(1H)-one core. A set of 32 N-alkylated/benzylated quinazoline derivatives were synthesized, characterized and evaluated for their inhibition against cholinesterases. N-alkylation of the series of the compounds reported previously (N-unsubstituted) resulted in improved activity. All the compounds showed inhibition of both enzymes in the micromolar to submicromolar range. Structure activity relationship (SAR) of the 32 derivatives showed that N-benzylated compounds possess good activity than N-alkylated compounds...
April 17, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28494853/in-vitro-antioxidant-assessment-and-a-rapid-hptlc-bioautographic-method-for-the-detection-of-anticholinesterase-inhibitory-activity-of-geophila-repens
#13
Umesh Chandra Dash, Atish Kumar Sahoo
OBJECTIVE: Geophila repens (L.) I. M. Johnst. (Rubiaceae), a small, creeping, perennial herb, is claimed to have memory-enhancing property. The goal of this study was to assess its antioxidant and anticholinesterase activity and conduct a rapid bioautographic enzyme assay for screening acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition of G. repens extracts. METHODS: Antioxidant activity of G. repens extracts was assessed by performing 1,1-diphenyl-2-picrylhydrazyl (DPPH), nitric oxide (NO), superoxide (SOD), hydroxyl (OH) and total antioxidant capacity (TAC) assays...
May 2017: Journal of Integrative Medicine
https://www.readbyqxmd.com/read/28494203/carbofuran-degraded-by-iron-doped-anatase-weakening-the-cholinesterase-inhibitory-activity-in-the-photoproducts-mixture
#14
Martín M Dávila-Jiménez, María P Elizalde-González, Esmeralda García-Díaz, Miguel González, M E Mendoza, M J Robles-Águila
Carbofuran is a toxic carbamate pesticide, and its use has increased in recent years. While marketing information indicates stability in different chemical media, carbofuran exhibits relative photolability. The aim of this research was to decompose carbofuran and to identify the photoproducts achieved when two different doped titania photocatalysts were employed under UV irradiation. The iron-doped TiO2 materials were obtained (a) via a hydrothermal method and (b) by an ultrasound-assisted sol-gel method. The precursors were TiOSO4⋅xH2O and Fe3(NO3)·9H2O...
May 11, 2017: Journal of Environmental Science and Health. Part. B, Pesticides, Food Contaminants, and Agricultural Wastes
https://www.readbyqxmd.com/read/28487125/design-synthesis-and-biological-evaluation-of-3-4-dihydro-2-1h-quinoline-o-alkylamine-derivatives-as-new-multipotent-cholinesterase-monoamine-oxidase-inhibitors-for-the-treatment-of-alzheimer-s-disease
#15
Zhipei Sang, Wanli Pan, Keren Wang, Qinge Ma, Lintao Yu, Wenmin Liu
A new family of multitarget molecules able to interact with acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as with monoamino oxidase (MAO) A and B, has been synthesized. Novel 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives have been designed using a conjunctive approach that combines the JMC49 and donepezil. The most promising compound TM-33 showed potent and balance inhibitory activities toward ChE and MAO (eeAChE, eqBuChE, hMAO-A and hMAO-B with IC50 values of 0.56μM, 2.3μM, 0...
April 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28485637/new-benz-imidazolopyridino-tacrines-as-nonhepatotoxic-cholinesterase-inhibitors-for-alzheimer-disease
#16
Houssem Boulebd, Lhassane Ismaili, Helene Martin, Alexandre Bonet, Mourad Chioua, José Marco Contelles, Ali Belfaitah
AIM: Due to the multifactorial nature of Alzheimer's disease, there is an urgent search for new more efficient, multitarget-directed drugs. RESULTS: This paper describes the synthesis, antioxidant and in vitro biological evaluation of ten (benz)imidazopyridino tacrines (7-16), showing less toxicity than tacrine at high doses, and potent cholinesterase inhibitory capacity, in the low micromolar range. Among them, compound 10 is a nonhepatotoxic tacrine at 1000 mM, showing moderate, but totally selective electric eel acetylcholinesterase inhibition, whereas molecule 16 is twofold less toxic than tacrine at 1000 μM, showing moderate and almost equipotent inhibition for electric eel acetylcholinesterase and equine butyrylcholinesterase...
May 9, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28485614/design-synthesis-molecular-modeling-and-anticholinesterase-activity-of-benzylidene-benzofuran-3-ones-containing-cyclic-amine-side-chain
#17
Farzad Mehrabi, Yaghoub Pourshojaei, Alireza Moradi, Mohammad Sharifzadeh, Leila Khosravani, Reyhaneh Sabourian, Samira Rahmani-Nezhad, Maryam Mohammadi-Khanaposhtani, Mohammad Mahdavi, Ali Asadipour, Hamid Reza Rahimi, Setareh Moghimi, Alireza Foroumadi
AIM: A series of 2-benzylidene-benzofuran-3-ones were designed from the structures of Ebselen analogs and aurone derivatives and synthesized in good yields. MATERIALS & METHODS: The target compounds were prepared by the condensation reaction between appropriate benzofuranones with amino alkoxy aldehydes and evaluated as cholinesterase inhibitors by Ellman's method. RESULTS: The in vitro anti-acetylcholinesterase (AChE)/butyrylcholinesterase activities of the synthesized compounds revealed that 7e (IC50 = 0...
May 9, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28483282/a-new-method-to-characterize-the-kinetics-of-cholinesterases-inhibited-by-carbamates
#18
Qiaoling Xiao, Huimin Zhou, Hong Wei, Huaqiao Du, Wen Tan, Yiyi Zhan, Marco Pistolozzi
The inhibition of cholinesterases (ChEs) by carbamates includes a carbamylation (inhibition) step, in which the drug transfers its carbamate moiety to the active site of the enzyme and a decarbamylation (activity recovery) step, in which the carbamyl group is hydrolyzed from the enzyme. The carbamylation and decarbamylation kinetics decide the extent and the duration of the inhibition, thus the full characterization of candidate carbamate inhibitors requires the measurement of the kinetic constants describing both steps...
April 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28468728/quantitative-estimation-of-cholinesterase-specific-drug-metabolism-of-carbamate-inhibitors-provided-by-the-analysis-of-the-area-under-the-inhibition-time-curve
#19
Huimin Zhou, Qiaoling Xiao, Wen Tan, Yiyi Zhan, Marco Pistolozzi
Several molecules containing carbamate groups are metabolized by cholinesterases. This metabolism includes a time-dependent catalytic step which temporary inhibits the enzymes. In this paper we demonstrate that the analysis of the area under the inhibition versus time curve (AUIC) can be used to obtain a quantitative estimation of the amount of carbamate metabolized by the enzyme. (R)-bambuterol monocarbamate and plasma butyrylcholinesterase were used as model carbamate-cholinesterase system. The inhibition of different concentrations of the enzyme was monitored for 5h upon incubation with different concentrations of carbamate and the resulting AUICs were analyzed...
April 9, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28467056/easy-preparable-butyrylcholinesterase-microgel-construct-for-facilitated-organophosphate-biosensing
#20
Larisa V Sigolaeva, Snezhana Yu Gladyr, Olga Mergel, Arjan P H Gelissen, Michael Noyong, Ulrich Simon, Dmitry V Pergushov, Ilya N Kurochkin, Felix A Plamper, Walter Richtering
A versatile guest matrix was fabricated from a temperature- and pH-sensitive poly(N-isopropylacrylamide)-co-(3-(N,N-dimethylamino)propylmethacrylamide) microgel (poly(NIPAM-co-DMAPMA), MG) for the gentle incorporation of butyrylcholinesterase (BChE). The microgel/BChE films were built up on a surface of graphite-based screen-printed electrodes (SPEs) premodified with MnO2 nanoparticles via a two-step sequential adsorption under careful temperature and pH control. On this basis, a rather simple amperometric biosensor construct was formed, which uses butyrylthiocholine as BChE substrate with subsequent MnO2-mediated thiocholine oxidation at a graphite-based SPE...
May 16, 2017: Analytical Chemistry
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