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https://www.readbyqxmd.com/read/27914011/activation-of-alpha-7-nicotinic-acetylcholine-receptor-reduces-brain-edema-in-mice-with-ischemic-stroke-and-bone-fracture
#1
Dingquan Zou, Man Luo, Zhenying Han, Lei Zhan, Wan Zhu, Shuai Kang, Chen Bao, Zhao Li, Jeffrey Nelson, Rui Zhang, Hua Su
Stroke is an important risk factor for bone fracture. We showed previously that bone fracture at the acute stage of ischemic stroke worsens, and activation of α-7 nicotinic acetylcholine receptor (α-7 nAchR) improves, stroke recovery by attenuating inflammation. We hypothesized that activation of α-7 nAchR also improves the blood-brain barrier (BBB) integrity. Permanent distal middle cerebral artery occlusion (pMCAO) was performed on C57BL/6J mice followed by tibia fracture 1 day later. Mice were treated with 0...
December 2, 2016: Molecular Neurobiology
https://www.readbyqxmd.com/read/27911341/longer-duration-of-mao-b-inhibitor-exposure-is-associated-with-less-clinical-decline-in-parkinson-s-disease-an%C3%A2-analysis%C3%A2-of%C3%A2-net-pd-ls1
#2
Robert A Hauser, Ruosha Li, Adriana Pérez, Xuehan Ren, Dan Weintraub, Jordan Elm, John L Goudreau, John C Morgan, John Y Fang, Michael J Aminoff, Chadwick W Christine, Rohit Dhall, Chizoba C Umeh, James T Boyd, Natividad Stover, Maureen Leehey, Richard M Zweig, Anthony P Nicholas, Ivan Bodis-Wollner, Allison Willis, Karl Kieburtz, Barbara C Tilley
BACKGROUND: Monoamine oxidase type B (MAO-B) inhibitors exhibit neuroprotective effects in preclinical models of PD but clinical trials have failed to convincingly demonstrate disease modifying benefits in PD patients. OBJECTIVE: To perform a secondary analysis of NET-PD LS1 to determine if longer duration of MAO-B inhibitor exposure was associated with less clinical decline. METHODS: The primary outcome measure was the Global Outcome (GO), comprised of 5 measures: change from baseline in the Schwab and England (ADL) scale, the 39-item Parkinson's Disease Questionnaire (PDQ-39), the UPDRS Ambulatory Capacity Scale, the Symbol Digit Modalities Test, and the most recent Modified Rankin Scale...
November 30, 2016: Journal of Parkinson's Disease
https://www.readbyqxmd.com/read/27908752/n-propargylpiperidines-with-naphthalene-2-carboxamide-or-naphthalene-2-sulfonamide-moieties-potential-multifunctional-anti-alzheimer-s-agents
#3
Urban Košak, Damijan Knez, Nicolas Coquelle, Boris Brus, Anja Pišlar, Florian Nachon, Xavier Brazzolotto, Janko Kos, Jacques-Philippe Colletier, Stanislav Gobec
In the brains of patients with Alzheimer's disease, the enzymatic activities of butyrylcholinesterase (BChE) and monoamine oxidase B (MAO-B) are increased. While BChE is a viable therapeutic target for alleviation of symptoms caused by cholinergic hypofunction, MAO-B is a potential therapeutic target for prevention of neurodegeneration in Alzheimer's disease. Starting with piperidine-based selective human (h)BChE inhibitors and propargylamine-based MAO inhibitors, we have designed, synthesized and biochemically evaluated a series of N-propargylpiperidines...
November 19, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27902880/monoamine-oxidase-inhibitory-activity-methyl-versus-chlorochalcone-derivatives
#4
Bijo Mathew, Gülberk Uçar, Githa Elizabeth Mathew, Sincy Mathew, Praseedha Kalatharakkal Purapurath, Fasil Moolayil, Smrithy Mohan, Sheeba Varghese Gupta
Numerous studies have shown that chalcones are promising scaffolds for the development of new monoamine oxidase-B (MAO-B) inhibitors. As a continuation of our ongoing research into the development of reversible human MAO-B (hMAO-B) inhibitors, two series of twenty chalcones containing electron-donating and electron-withdrawing substituents were synthesized. All compounds were found to be competitive, selective, and reversible inhibitors of hMAO-B except (2E)-1-(4-methylphenyl)-3-(4-nitrophenyl)prop-2-en-1-one (P7) and (2E)-1-(4-chlorophenyl)-3-(4-nitrophenyl)prop-2-en-1-one (P17), which were found to be selective inhibitors of hMAO-A...
November 30, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27896136/attention-deficit-hyperactivity-disorder-suffers-from-mitochondrial-dysfunction
#5
Poonam Verma, Alpana Singh, Dominic Ngima Nthenge-Ngumbau, Usha Rajamma, Swagata Sinha, Kanchan Mukhopadhyay, Kochupurackal P Mohanakumar
BACKGROUND: Pathophysiology of attention-deficit hyperactivity disorder (ADHD) is not known, and therefore the present study investigated mitochondrial defects, if any in cybrids created from patients and control population. METHODS: To investigate mitochondrial pathology in ADHD, cybrids cell lines were created from ADHD probands and controls by fusing their platelets with ρ(0)-cells prepared from SH-SY5Y neuroblastoma cell line. Cellular respiration, oxidative stress, mitochondrial membrane potential and morphology were evaluated employing oxygraph, mitochondria-specific fluorescence staining and evaluation by FACS, and immunocytochemistry...
December 2016: BBA Clinical
https://www.readbyqxmd.com/read/27863747/symmetrical-aryl-linked-bis-iminothiazolidinones-as-new-chemical-entities-for-the-inhibition-of-monoamine-oxidases-synthesis-in-vitro-biological-evaluation-and-molecular-modelling-analysis
#6
Naeem Abbas, Sumera Zaib, Syeda Mahwish Bakht, Aliya Ibrar, Imtiaz Khan, Sadaf Batool, Aamer Saeed, Jamshed Iqbal
The multifactorial nature of Parkinson's disease necessitates the development of new chemical entities with inherent ability to address key pathogenic processes. To this end, two series of new symmetrical 1,2- and 1,4-bis(2-aroyl/alkoylimino-5-(2-methoxy-2-oxoethylidene)-4-oxo-thiazolidin-3-yl)benzene derivatives (3a-g and 5a-e) were synthesized in good yields by the cyclization of 1,2- and 1,4-bis(N'-substituted thioureido)benzene intermediates with dimethyl acetylenedicarboxylate (DMAD) in methanol at ambient temperature...
November 9, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27855360/benzyloxynitrostyrene-analogues-a-novel-class-of-selective-and-highly-potent-inhibitors-of-monoamine-oxidase-b
#7
Mietha M Van der Walt, Gisella Terre'Blanche, Jacobus P Petzer, Anél Petzer
This study examines a series of novel 3-benzyloxy-β-nitrostyrene analogues as a novel class of inhibitors of the monoamine oxidase (MAO) enzymes. MAO inhibitors are considered useful for the treatment of depression and Parkinson's disease, and have recently attracted attention as potential therapeutic agents for a range of disorders including Alzheimer's disease, prostate cancer and certain cardiomyopathies. This study shows that the 3-benzyloxy-β-nitrostyrene analogues are potent inhibitors of the MAO-B isoform with IC50 values in the nanomolar range (39-565 nM)...
November 9, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27845365/computational-drug-target-screening-through-protein-interaction-profiles
#8
Santiago Vilar, Elías Quezada, Eugenio Uriarte, Stefano Costanzi, Fernanda Borges, Dolores Viña, George Hripcsak
The development of computational methods to discover novel drug-target interactions on a large scale is of great interest. We propose a new method for virtual screening based on protein interaction profile similarity to discover new targets for molecules, including existing drugs. We calculated Target Interaction Profile Fingerprints (TIPFs) based on ChEMBL database to evaluate drug similarity and generated new putative compound-target candidates from the non-intersecting targets in each pair of compounds. A set of drugs was further studied in monoamine oxidase B (MAO-B) and cyclooxygenase-1 (COX-1) enzyme through molecular docking and experimental assays...
November 15, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27806193/neuroprotective-effect-of-a-new-7-8-dihydroxycoumarin-based-fe2-cu2-chelator-in-cell-and-animal-models-of-parkinson-s-disease
#9
Pabla Aguirre, Olimpo García-Beltrán, Victoria Tapia, Yorka Muñoz, Bruce Kennedy Cassels, Marco T Nunez
Disturbed iron homeostasis, often coupled to mitochondrial dysfunction, plays an important role in the progression of common neurodegenerative diseases such as Parkinson disease (PD). Recent studies have underlined the relevance of iron chelation therapy for the treatment of these diseases. Here we describe the synthesis, chemical and biological characterization of the multifunctional chelator 7,8-dihydroxy-4-((methylamino)methyl)-2H-chromen-2-one (DHC12). Metal selectivity of DHC12 was Cu2+ ̴ Fe2+ > Zn2+ > Fe3+...
November 2, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27803666/inhibitors-of-mao-a-and-mao-b-in-psychiatry-and-neurology
#10
REVIEW
John P M Finberg, Jose M Rabey
Inhibitors of MAO-A and MAO-B are in clinical use for the treatment of psychiatric and neurological disorders respectively. Elucidation of the molecular structure of the active sites of the enzymes has enabled a precise determination of the way in which substrates and inhibitor molecules are metabolized, or inhibit metabolism of substrates, respectively. Despite the knowledge of the strong antidepressant efficacy of irreversible MAO inhibitors, their clinical use has been limited by their side effect of potentiation of the cardiovascular effects of dietary amines ("cheese effect")...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27777099/longevity-study-with-low-doses-of-selegiline-deprenyl-and-2r-1-1-benzofuran-2-yl-n-propylpentane-2-amine-bpap
#11
J Knoll, I Miklya
AIMS: The first longevity study demonstrating that rats treated with the MAO-B inhibitory dose of (-)-deprenyl (0.25mg/kg) lived significantly longer than their saline-treated peers was published in 1988, and corroborated in many papers. The recent findings that (-)-deprenyl is primarily a PEA-derived synthetic catecholaminergic activity enhancersubstance; (2R)-1-(1-benzofuran-2-yl)-N-propylpentane-2-amine (BPAP) is a tryptamine-derived synthetic enhancer substance, initiated our first longevity study on rats with low enhancer doses of (-)-deprenyl and BPAP to test the enhancer effect's role inlife extension...
October 21, 2016: Life Sciences
https://www.readbyqxmd.com/read/27754693/isolation-of-acacetin-from-calea-urticifolia-with-inhibitory-properties-against-human-monoamine-oxidase-a-and-b
#12
Narayan D Chaurasiya, Vedanjali Gogineni, Khaled M Elokely, Francisco León, Marvin J Núñez, Michael L Klein, Larry A Walker, Stephen J Cutler, Babu L Tekwani
Calea urticifolia (Asteraceae: Asteroideae) has long been used as a traditional medicine in El Salvador to treat arthritis and fever, among other illnesses. The chloroform extract of the leaves of C. urticifolia showed potent inhibition of recombinant human monoamine oxidases (MAO-A and -B). Further bioassay-guided fractionation led to the isolation of a flavonoid, acacetin, as the most prominent MAO inhibitory constituent, with IC50 values of 121 and 49 nM for MAO-A and -B, respectively. The potency of MAO inhibition by acacetin was >5-fold higher for MAO-A (0...
October 18, 2016: Journal of Natural Products
https://www.readbyqxmd.com/read/27747875/identification-of-compounds-from-non-polar-fractions-of-blechnum-spp-and-a-multitarget-approach-involving-enzymatic-modulation-and-oxidative-stress
#13
Juliana Maria de Mello Andrade, Natasha Maurmann, Patricia Pranke, Izabel Cristina Casanova Turatti, Norberto Peporine Lopes, Amélia T Henriques
OBJECTIVES: The hexane (HEX) and dichloromethane (DCM) fractions from Blechnum binervatum, Blechnum brasiliense and Blechnum occidentale were studied about phytochemicals and biological properties using multitarget approach. METHODS: The chemical composition was performed by gas chromatography coupled with mass spectrometry detector (GC-MS) analysis. Antioxidant capacity was evaluated against free radicals and on lipid peroxidation. Monoamine oxidases (MAO) and cholinesterases enzymatic modulation, as well as effects on rat and human cells, were assessed...
October 17, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27744252/synthesis-and-evaluation-of-7-substituted-coumarin-derivatives-as-multimodal-monoamine-oxidase-b-and-cholinesterase-inhibitors-for-the-treatment-of-alzheimer-s-disease
#14
Jacques Joubert, Germaine B Foka, Benjamin P Repsold, Douglas W Oliver, Erika Kapp, Sarel F Malan
A series of 7-substituted coumarin derivatives were designed and synthesised to display ChE and MAO-B inhibitory activity. The compounds consisted out of a coumarin structure (MAO-B inhibitor) and benzyl-, piperidine-, N-benzylpiperidine- or p-bromo-N-benzylpiperizine moiety, resembling the N-benzylpiperidine function of donepezil (ChE inhibitor), connected via an alkyl ether linkage at the 7 position. The biological assay results indicated that all the compounds (1-25) displayed selective inhibition to hMAO-B over hMAO-A, with the benzyloxy series (1-8, 10-13) showing nano-molar hMAO-B inhibition (IC50: 0...
September 15, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27734680/empirical-valence-bond-simulations-of-the-hydride-transfer-step-in-the-monoamine-oxidase-a-catalyzed-metabolism-of-noradrenaline
#15
Matic Poberznik, Miha Purg, Matej Repič, Janez Mavri, Robert Vianello
Monoamine oxidases (MAOs) A and B are flavoenzymes responsible for the metabolism of biogenic amines such as dopamine, serotonin and noradrenaline, which is why they have been extensively implicated in the etiology and course of various neurodegenerative disorders, and, accordingly, used as primary pharmacological targets to treat these debilitating cognitive diseases. The precise chemical mechanism through which MAOs regulate the amine concentration, which is vital for the development of novel inhibitors, is still not unambiguously determined in the literature...
October 13, 2016: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/27725503/2-azolylchromone-derivatives-as-potent-and-selective-inhibitors-of-monoamine-oxidases-a-and-b
#16
Koichi Takao, Takayuki Saito, Daisuke Chikuda, Yoshiaki Sugita
A series of 2-azolylchromone derivatives were synthesized and their monoamine oxidase (MAO) A and B inhibitory activities were evaluated. Of the synthesized compounds, compounds 1b, 2b, 4a-c, 5b and 7b showed potent inhibitory activities against MAO-A (IC50 values, 1b: 0.32 µM; 2b: 0.14 µM; 4a: 0.11 µM; 4b: 0.023 µM; 4c: 0.15 µM; 5b: 0.59 µM; 7b: 0.19 µM) and 4a, c, 5a, c, 6c and 8c for MAO-B (IC50 values, 4a: 0.028 µM; 4c: 0.019 µM; 5a: 0.73 µM; 5c: 0.28 µM; 6c: 0.28 µM; 8c: 0...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27715253/an-overview-of-analytical-methods-for-the-determinationof-monoamine-oxidase-inhibitors-in-pharmaceutical-formulations-and-biological-fluids
#17
Cafer Saka
Monoamine oxidase inhibitors (MAOIs) were the first type of antidepressant developed. MAOIs elevate the levels of norepinephrine, serotonin, and dopamine by inhibiting an enzyme called monoamine oxidase. They are also used in the treatment of Parkinson's disease, tuberculosis, and several other disorders. Therefore, it is very important to develop efficient analytical methods for monitoring and management. There are two isoforms of monoamine oxidase, MAO-A and MAO-B. In this article, analyses of MAOIs in pharmaceutical formulations and biological fluids were reviewed from 2000 to the present, including all types of chromatographic, spectrophotometric, electrophoretic, and voltammetric techniques, focusing on isoniazid, tranylcypromine, moclobemide, rasagiline, and selegiline...
October 7, 2016: Critical Reviews in Analytical Chemistry
https://www.readbyqxmd.com/read/27676470/new-isoxazolidinone-and-3-4-dehydro-%C3%AE-proline-derivatives-as-antibacterial-agents-and-mao-inhibitors-a-complex-balance-between-two-activities
#18
Lucia Ferrazzano, Angelo Viola, Elena Lonati, Alessandra Bulbarelli, Rosario Musumeci, Clementina Cocuzza, Marco Lombardo, Alessandra Tolomelli
Among the different classes of antibiotics, oxazolidinone derivatives represent important drugs, since their unique mechanism of action overcomes commonly diffused multidrug-resistant bacteria. Anyway, the structural similarity of these molecules to monoamino oxidase (MAO) inhibitors, like toloxatone and blefoxatone, induces in many cases loss of selectivity as a major concern. A small library of compounds based on isoxazolidinone and dehydro-β-proline scaffold was designed with the aim to obtain antibacterial agents, evaluating at the same time the potential effects of structural features on MAO inhibitory behaviour...
September 4, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27666135/rapid-synthesis-of-flavone-based-monoamine-oxidase-mao-inhibitors-targeting-two-active-sites-using-click-chemistry
#19
Wei Zhen Jia, Feng Cheng, Yin Jun Zhang, Jin Yan Ge, Shao Q Yao, Qing Zhu
A new library of flavone derivatives targeting two active sites of monoamine oxidases ("aromatic cage" and substrate cavity) were designed and synthesized using click chemistry (CuAAC reaction) between 6-N3 -2-phenyl chromones (Az1-Az2) and a series of alkynes (k1-k20). Their inhibitory activities against MAO isoforms (MAO-A and MAO-B) are evaluated. Compounds with fluorine, amide bonds, or amino bonds have shown better inhibition. The most potent flavone MAO inhibitor studied is Az2k19 (1.6 μm for MAO-A, 2...
September 26, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27662218/2-heteroarylidene-1-indanone-derivatives-as-inhibitors-of-monoamine-oxidase
#20
Magdalena S Nel, Anél Petzer, Jacobus P Petzer, Lesetja J Legoabe
In the present study a series of fifteen 2-heteroarylidene-1-indanone derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. These compounds are structurally related to series of heterocyclic chalcone derivatives which have previously been shown to act as MAO-B specific inhibitors. The results document that the 2-heteroarylidene-1-indanones are in vitro inhibitors of MAO-B, displaying IC50 values of 0.0044-1.53μM. Although with lower potencies, the derivatives also inhibit the MAO-A isoform with IC50 values as low as 0...
September 17, 2016: Bioorganic Chemistry
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