Cholinesterase Inhibitors
Mostrando 1-12 de 40 artigos, teses e dissertações.
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1. An Expedient Synthesis of Tacrine-Squaric Hybrids as Potent, Selective and Dual-Binding Cholinesterase Inhibitors
The restoration of acetylcholine levels in the brain by inhibition of cholinesterases is currently the most successful therapeutic strategy to treat neurodegenerative disorders. In this context, tacrine has been largely investigated as a starting scaffold for the development of promising new anticholinesterases compounds for the treatment of neurodegenerativ
J. Braz. Chem. Soc.. Publicado em: 2020-05
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2. Chiral Bistacrine Analogues: Synthesis, Cholinesterase Inhibitory Activity and a Molecular Modeling Approach
Cholinesterase enzymes are important targets for the therapy of Alzheimer’s disease. Tacrine-based dual binding site cholinesterases inhibitors are potential disease-modifying anti-Alzheimer drug candidates. In the present work, we described the synthesis of a series of chiral homo- and heterodimers of bis(7)-tacrine connected by a heptylene chain as a spa
J. Braz. Chem. Soc.. Publicado em: 2017-11
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3. Aminonaphthoquinone Mannich Bases Derived from Lawsone and Their Copper(II) Complex Derivatives: Synthesis and Potential Cholinesterase Inhibitors as Identified by On-flow Assay
A new series of Mannich bases derived from 2-hydroxy-1,4-naphthoquinone (lawsone), substituted benzaldehydes and two primary amines, and their Cu2+ complexes were synthesized and evaluated for their potential as selective cholinesterase inhibitors (ChEIs). Immobilized capillary enzyme reactors (ICERs) bearing butyrylcholinesterase (BChE) and acetylcholineste
J. Braz. Chem. Soc.. Publicado em: 2016-03
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4. Modelagem MIA-QSAR de inibidores de acetilcolinesterase= : MIA-QSAR modeling of inhibitors actylcholinesterase / MIA-QSAR modeling of inhibitors actylcholinesterase
O presente trabalho trata de um estudo sobre compostos que se comportam como inibidores da acetilcolinesterase, uma importante enzima do processo de cognição. A acetilcolinesterase atua na hidrólise da acetilcolina, responsável pela comunicação entre os neurônios. Uma das modalidades para o design racional de fármacos é a estimativa de propriedades
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 04/09/2012
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5. Synthesis of compounds with potential anticholinesterase activity / Sínteses de compostos com potencial atividade anticolinesterásica
Este trabalho descreve um estudo teórico-experimental envolvendo derivados da Piridostigmina e do Edrofônio, que possuem ação como inibidores da enzima acetilcolinesterase. Os anticolinesterásicos são utilizados como medicamento para o tratamento do Mal de Alzheimer. Primeiramente foram sintetizados os derivados da Piridostigmina (brometo de N,N-dimeti
IBICT - Instituto Brasileiro de Informação em Ciência e Tecnologia. Publicado em: 01/07/2011
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6. Estudos de modelagem molecular e relação estrutura-atividade da acetilcolinesterase e inibidores em Mal de Alzheimer / Molecular modeling studies and structure-activity relationships of acetylcholinesterase inhibitors in Alzheimers disease.
Alzheimers disease is the leading cause of dementia in the elderly. The progression of symptoms is associated with structural changes in cholinergic synapses in specific brain regions and consequentely to decrease the potential of cholinergic neurotransmission. Thus, the increased capacity of cholinergic neurotransmission is the fundamental mechanism of the
Publicado em: 2011
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7. Acute electrophysiologic consequences of pyridostigmine inhibition of cholinesterase in humans
The cardiovascular electrophysiologic basis for the action of pyridostigmine, an acetylcholinesterase inhibitor, has not been investigated. The objective of the present study was to determine the cardiac electrophysiologic effects of a single dose of pyridostigmine bromide in an open-label, quasi-experimental protocol. Fifteen patients who had been indicated
Publicado em: 2011
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8. Efeitos pré e pós sinápticos dos inibidores da acetilcolinesterase na neurotransmissão em musculatura lisa.
Justification: The present work considers the effects of new inhibitors of acetylcholinesterase (AChE) on the reactivity and neurotransmission in rats and mice. The new anticholinesterase compounds, ITH12118 and ITH12117, have an hybrid stucture, derived from the molecule of of the anticholinesterase Tacrine and the 1,4 dihydropyridine nimodipine, a blocker
Publicado em: 2010
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9. KRAIT VENOM ACETYLCHOLINESTERASE IS A SUITABLE CANDIDATE FOR BIOCHEMICAL ANALYSIS: CHARACTERIZATION AND COMPARATIVE INHIBITORY STUDIES / CARACTERIZAÇÃO DA ATIVIDADE DA ENZIMA ACETILCOLINESTERASE DE VENENO DE Bungarus sindanus: ESTUDOS COMPARATIVOS
A enzima acetilcolinesterase (AChE, E.C. 3.1.1.7) faz parte de uma família distinta de serina hidrolases, sendo uma importante enzima regulatória, encontrada principalmente no encéfalo, músculos, eritrócitos, neurônios colinérgicos e também em veneno de cobra. Nas sinapses, a sua principal função é a hidrólise no neutrotransmissor acetilcolina (A
Publicado em: 2008
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10. Ric-8B, a putative GEF for Galpha-olf, promotes functional expression of odorant receptors / Ric-8B, um provável GEF para Galpha-olf, promove expressão funcional de receptores olfatórios
Os odores são detectados por uma grande família de receptores olfatórios (ORs) que são expressos nos neurônios olfatórios localizados no nariz. Os ORs ativados por um determinado odor acoplam-se à proteína Galfaolf que irá promover a ativação da adenilil ciclase III, resultando na produção de AMPc. O aumento da concentração de AMPc irá ativar
Publicado em: 2006
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11. Produtos naturais como candidatos a fármacos úteis no tratamento do Mal de Alzheimer
Alzheimer's disease (AD) is a progressive neurodegenerative pathology with severe economic and social impact. There is currently no cure, although cholinesterase inhibitors provide effective temporary relief of symptoms in some patients. Nowadays drug research and development are based on the cholinergic hypothesis that supports the cognition improvement by
Química Nova. Publicado em: 2004-08
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12. Ivermectin resistant and susceptible third-stage larvae of Haemonchus contortus: cholinesterase and phosphatase activities
Cholinesterase and acid phosphatase (AP), but not alkaline phosphatase activities, were detected in cytosolic and membrane-bound fractions of ivermectin resistant and susceptible Haemonchus contortus infective-stage larvae. Some differences in acetylcholinesterase activity of cytosolic fractions and in the AP activity of these fractions as well as in the res
Memórias do Instituto Oswaldo Cruz. Publicado em: 2004-03