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[PMID]:28728104
[Au] Autor:Yang HL; Cai P; Liu QH; Yang XL; Li F; Wang J; Wu JJ; Wang XB; Kong LY
[Ad] Endereço:School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China; Jiangsu Key Laboratory of Bioactive Natural Product Research and State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 21
[Ti] Título:Design, synthesis and evaluation of coumarin-pargyline hybrids as novel dual inhibitors of monoamine oxidases and amyloid-ß aggregation for the treatment of Alzheimer's disease.
[So] Source:Eur J Med Chem;138:715-728, 2017 Sep 29.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A series of coumarin-pargyline hybrids (4a-x) have been designed, synthesized and evaluated as novel dual inhibitors of Alzheimer's disease (AD). Most of the compounds exhibited a potent ability to inhibit amyloid-ß (Aß) aggregation and monoamine oxidases. In particular, compound 4x exhibited remarkable inhibitory activities against monoamine oxidases (IC , 0.027 ± 0.004 µM for MAO-B; 3.275 ± 0.040 µM for MAO-A) and Aß aggregation (54.0 ± 1.1%, 25 µM). Moreover, compound 4x showed low toxicity according to in vitro cell toxicity test. The results of the parallel artificial membrane permeability assay for blood-brain barrier indicated that compound 4x would be potent to cross the blood-brain barrier. Collectively, these findings demonstrate that compound 4x was an effective and promising candidate for AD therapy.
[Mh] Termos MeSH primário: Doença de Alzheimer/tratamento farmacológico
Peptídeos beta-Amiloides/antagonistas & inibidores
Cumarínicos/farmacologia
Inibidores da Monoaminoxidase/farmacologia
Monoaminoxidase/metabolismo
Pargilina/farmacologia
[Mh] Termos MeSH secundário: Doença de Alzheimer/metabolismo
Peptídeos beta-Amiloides/metabolismo
Animais
Sobrevivência Celular/efeitos dos fármacos
Cumarínicos/química
Relação Dose-Resposta a Droga
Desenho de Drogas
Seres Humanos
Masculino
Camundongos
Camundongos Endogâmicos
Estrutura Molecular
Inibidores da Monoaminoxidase/síntese química
Inibidores da Monoaminoxidase/química
Células PC12
Pargilina/química
Agregados Proteicos/efeitos dos fármacos
Ratos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amyloid beta-Peptides); 0 (Coumarins); 0 (Monoamine Oxidase Inhibitors); 0 (Protein Aggregates); 9MV14S8G3E (Pargyline); A4VZ22K1WT (coumarin); EC 1.4.3.4 (Monoamine Oxidase)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171002
[Lr] Data última revisão:
171002
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170721
[St] Status:MEDLINE


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[PMID]:28377178
[Au] Autor:Huang M; Chen C; Geng J; Han D; Wang T; Xie T; Wang L; Wang Y; Wang C; Lei Z; Chu X
[Ad] Endereço:Department of Medical Oncology, Jinling Hospital, School of Medicine, Nanjing University, Nanjing, Jiangsu Province, People's Republic of China.
[Ti] Título:Targeting KDM1A attenuates Wnt/ß-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma.
[So] Source:Cancer Lett;398:12-21, 2017 Jul 10.
[Is] ISSN:1872-7980
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Use of the tyrosine kinase inhibitor sorafenib in patients with advanced hepatocellular carcinoma (HCC) is often hindered by the development of resistance, which has been recently shown to be associated with the emergence of a cancer stem cell (CSC) subpopulation. However, it remains largely unknown whether epigenetic mechanisms, especially histone posttranslational modifications, are causally linked to the maintenance of stem-like properties in sorafenib-resistant HCC. In this study, we report that the activity of lysine-specific histone demethylase 1A (KDM1A or LSD1) is required for the emergence of cancer stem cells following prolonged sorafenib treatment. As such, KDM1A inhibitors, such as pargyline and GSK2879552, dramatically suppress stem-like properties of sorafenib-resistant HCC cells. Mechanistically, KDM1A inhibitors derepress the expression of multiple upstream negative regulators of the Wnt signaling pathway to downregulate the ß-catenin pathway. More importantly, KDM1A inhibition resensitizes sorafenib-resistant HCC cells to sorafenib in vivo, at least in part through reducing a CSC pool, suggesting a promising opportunity for this therapeutic combination. Together, these findings suggest that KDM1A inhibitors may be utilized to alleviate acquired resistance to sorafenib, thus increasing the therapeutic efficacy of sorafenib in HCC patients.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia
Benzoatos/farmacologia
Carcinoma Hepatocelular/tratamento farmacológico
Ciclopropanos/farmacologia
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Histona Desmetilases/antagonistas & inibidores
Neoplasias Hepáticas/tratamento farmacológico
Células-Tronco Neoplásicas/efeitos dos fármacos
Niacinamida/análogos & derivados
Pargilina/farmacologia
Compostos de Fenilureia/farmacologia
Inibidores de Proteínas Quinases/farmacologia
Via de Sinalização Wnt/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Carcinoma Hepatocelular/enzimologia
Carcinoma Hepatocelular/genética
Carcinoma Hepatocelular/patologia
Linhagem Celular Tumoral
Histona Desmetilases/genética
Histona Desmetilases/metabolismo
Seres Humanos
Neoplasias Hepáticas/enzimologia
Neoplasias Hepáticas/genética
Neoplasias Hepáticas/patologia
Masculino
Camundongos Nus
Terapia de Alvo Molecular
Células-Tronco Neoplásicas/enzimologia
Células-Tronco Neoplásicas/patologia
Niacinamida/farmacologia
Fenótipo
Interferência de RNA
Fatores de Tempo
Transfecção
Carga Tumoral/efeitos dos fármacos
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Benzoates); 0 (Cyclopropanes); 0 (GSK2879552); 0 (Phenylurea Compounds); 0 (Protein Kinase Inhibitors); 25X51I8RD4 (Niacinamide); 9MV14S8G3E (Pargyline); 9ZOQ3TZI87 (sorafenib); EC 1.14.11.- (Histone Demethylases); EC 1.5.- (KDM1A protein, human)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170821
[Lr] Data última revisão:
170821
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170406
[St] Status:MEDLINE


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[PMID]:27793854
[Au] Autor:Du CK; Zhan DY; Akiyama T; Inagaki T; Shishido T; Shirai M; Pearson JT
[Ad] Endereço:Department of Cardiac Physiology, National Cerebral and Cardiovascular Center Research Institute, Osaka, Japan; and duchk@ncvc.go.jp.
[Ti] Título:Myocardial interstitial levels of serotonin and its major metabolite 5-hydroxyindole acetic acid during ischemia-reperfusion.
[So] Source:Am J Physiol Heart Circ Physiol;312(1):H60-H67, 2017 Jan 01.
[Is] ISSN:1522-1539
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The aim of this study was to examine the accumulation of serotonin (5-HT) and degradation of 5-HT taken up into cells in the ischemic region during myocardial ischemia-reperfusion. Using microdialysis technique in anesthetized rats, we monitored myocardial interstitial levels of 5-HT and its metabolite produced by monoamine oxidase (MAO), 5-hydroxyindole acetic acid (5-HIAA), during 30-min coronary occlusion followed by 45-min reperfusion, and investigated the effects of local administration of the MAO inhibitor pargyline and the 5-HT uptake inhibitor fluoxetine. In the vehicle group, the dialysate 5-HT concentration increased from 1.3 ± 0.2 nM at baseline to 29.6 ± 2.8 nM at 22.5-30 min of occlusion, but the dialysate 5-HIAA concentration did not change from baseline (9.9 ± 1.1 nM). Upon reperfusion, the dialysate 5-HT concentration increased further to a peak (34.2 ± 4.2 nM) at 0-7.5 min and then declined. The dialysate 5-HIAA concentration increased to 31.9 ± 5.2 nM at 7.5-15 min of reperfusion and maintained this high level until 45 min. Pargyline markedly suppressed the increase in dialysate 5-HIAA concentration after reperfusion and increased the averaged dialysate 5-HT concentration during the reperfusion period. Fluoxetine suppressed the increase in dialysate 5-HT concentration during occlusion but did not change dialysate 5-HT or 5-HIAA concentration after reperfusion. During ischemia, 5-HT secreted from ischemic tissues accumulates but 5-HT degradation by MAO is suppressed. After reperfusion, degradation of 5-HT taken up into cells is enhanced and contributes to the clearance of accumulated 5-HT. This degradation following cellular uptake is dependent on MAO activity but not the fluoxetine-sensitive uptake transporter. NEW & NOTEWORTHY: By monitoring myocardial interstitial levels of 5-HT and its metabolite, 5-hydroxyindole acetic acid, we investigated 5-HT kinetics during myocardial ischemia-reperfusion. 5-HT accumulates but 5-HT degradation is suppressed during ischemia. After reperfusion, 5-HT degradation is enhanced and this degradation is dependent on monoamine oxidase activity but not fluoxetine-sensitive uptake transporter.
[Mh] Termos MeSH primário: Oclusão Coronária/metabolismo
Ácido Hidroxi-Indolacético/metabolismo
Traumatismo por Reperfusão Miocárdica/metabolismo
Miocárdio/metabolismo
Serotonina/metabolismo
[Mh] Termos MeSH secundário: Animais
Fluoxetina/farmacologia
Masculino
Microdiálise
Monoaminoxidase/metabolismo
Inibidores da Monoaminoxidase/farmacologia
Pargilina/farmacologia
Ratos
Ratos Wistar
Inibidores da Captação de Serotonina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Monoamine Oxidase Inhibitors); 0 (Serotonin Uptake Inhibitors); 01K63SUP8D (Fluoxetine); 333DO1RDJY (Serotonin); 54-16-0 (Hydroxyindoleacetic Acid); 9MV14S8G3E (Pargyline); EC 1.4.3.4 (Monoamine Oxidase)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170626
[Lr] Data última revisão:
170626
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161030
[St] Status:MEDLINE
[do] DOI:10.1152/ajpheart.00471.2016


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[PMID]:27404955
[Au] Autor:Jelen M; Pluta K; Zimecki M; Morak-Mlodawska B; Artym J; Kocieba M; Kochanowska I
[Ad] Endereço:a Department of Organic Chemistry , School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia , Sosnowiec , Katowice , Poland and.
[Ti] Título:Synthesis and biological evaluation of novel propargylquinobenzothiazines and their derivatives as potential antiproliferative, anti-inflammatory, and anticancer agents.
[So] Source:J Enzyme Inhib Med Chem;31(sup3):83-88, 2016.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Azaphenothiazines containing the quinoline ring, 8-10-substituted 6H-quinobenzothiazines and 6H-diquinothiazine were transformed into new 6-propargyl and 6-dialkylaminobutynyl derivatives containing the triple bond. Most of them displayed strong antiproliferative actions against human peripheral blood mononuclear cells (PBMC) stimulated with phytohemagglutinin A (PHA), strongly suppressed lipopolysaccharide (LPS)-induced TNF-α production by whole blood human cell cultures, and exhibited low cytotoxicity. Three propargylquinobenzothiazines with the bromine, trifluoromethyl, and methylthio groups at position 9 and propargyldiquinothiazine exhibited comparable actions to cisplatin against the L-1210 and SW-948 tumor lines. 6-Propargyl-9-trifluoromethylquinobenzothiazine was shown to block caspase 3 expression and inhibit expression of caspase 8 and 9 in Jurkat cells indicating its possible mechanism of action. These derivatives could be promising, potential therapeutics for treatment of neoplastic diseases and autoimmune disorders.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Antineoplásicos/farmacologia
Doenças Autoimunes/tratamento farmacológico
Leucócitos Mononucleares/efeitos dos fármacos
Neoplasias/tratamento farmacológico
Pargilina/farmacologia
Tiazinas/farmacologia
[Mh] Termos MeSH secundário: Anti-Inflamatórios não Esteroides/química
Anti-Inflamatórios não Esteroides/isolamento & purificação
Antineoplásicos/química
Antineoplásicos/isolamento & purificação
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Estrutura Molecular
Neoplasias/patologia
Pargilina/síntese química
Pargilina/química
Relação Estrutura-Atividade
Tiazinas/síntese química
Tiazinas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antineoplastic Agents); 0 (Thiazines); 9MV14S8G3E (Pargyline)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170223
[Lr] Data última revisão:
170223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160713
[St] Status:MEDLINE


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[PMID]:27399662
[Au] Autor:Mancuso R; Maner A; Ziccarelli I; Pomelli C; Chiappe C; Della Ca' N; Veltri L; Gabriele B
[Ad] Endereço:Laboratory of Industrial and Synthetic Organic Chemistry (LISOC), Department of Chemistry and Chemical Technologies, University of Calabria, Via Pietro Bucci 12/C, 87036 Arcavacata di Rende (CS), Italy. raffaella.mancuso@unical.it.
[Ti] Título:Auto-Tandem Catalysis in Ionic Liquids: Synthesis of 2-Oxazolidinones by Palladium-Catalyzed Oxidative Carbonylation of Propargylic Amines in EmimEtSO4.
[So] Source:Molecules;21(7), 2016 Jul 08.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:A convenient carbonylative approach to 2-oxazolidinone derivatives carried out using an ionic liquid (1-ethyl-3-methylimidazolium ethyl sulfate, EmimEtSO4) as the solvent is presented. It is based on the sequential concatenation of two catalytic cycles, both catalyzed by the same metal species (auto-tandem catalysis): the first cycle corresponds to the oxidative monoaminocarbonylation of the triple bond of propargylic amines to give the corresponding 2-ynamide intermediates, while the second one involves the cyclocarbonylation of the latter to yield 2-(2-oxooxazolidin-5-ylidene)-acetamides. Reactions are carried out using a simple catalytic system consisting of PdI2 in conjunction with an excess of KI, and the catalyst/solvent system could be recycled several times without appreciable loss of activity after extraction of the organic product with Et2O.
[Mh] Termos MeSH primário: Imidazóis/química
Líquidos Iônicos/química
Oxazolidinonas/síntese química
Paládio/química
Pargilina/análogos & derivados
Propilaminas/química
[Mh] Termos MeSH secundário: Acetamidas/síntese química
Catálise
Ciclização
Oxirredução
Pargilina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acetamides); 0 (Imidazoles); 0 (Ionic Liquids); 0 (Oxazolidinones); 0 (Propylamines); 2450-71-7 (propargylamine); 5TWQ1V240M (Palladium); 9MV14S8G3E (Pargyline); TVE1D62MAK (1-ethyl-3-methylimidazolium)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160712
[St] Status:MEDLINE


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[PMID]:27396685
[Au] Autor:Di Pietro O; Alencar N; Esteban G; Viayna E; Szalaj N; Vázquez J; Juárez-Jiménez J; Sola I; Pérez B; Solé M; Unzeta M; Muñoz-Torrero D; Luque FJ
[Ad] Endereço:Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia and Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Joan XXIII 27-31, E-08028 Barcelona, Spain.
[Ti] Título:Design, synthesis and biological evaluation of N-methyl-N-[(1,2,3-triazol-4-yl)alkyl]propargylamines as novel monoamine oxidase B inhibitors.
[So] Source:Bioorg Med Chem;24(20):4835-4854, 2016 Oct 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Different azides and alkynes have been coupled via Cu-catalyzed 1,3-dipolar Huisgen cycloaddition to afford a novel family of N - and C -substituted 1,2,3-triazole derivatives that feature the propargylamine group typical of irreversible MAO-B inhibitors at the C4-side chain of the triazole ring. All the synthesized compounds were evaluated against human MAO-A and MAO-B. Structure-activity relationships and molecular modeling were utilized to gain insight into the structural and chemical features that enhance the binding affinity and selectivity between the two enzyme isoforms. Several lead compounds, in terms of potency (submicromolar to low micromolar range), MAO-B selective recognition, and brain permeability, were identified. One of these leads (MAO-B IC of 3.54µM, selectivity MAO-A/MAO-B index of 27.7) was further subjected to reversibility and time-dependence inhibition studies, which disclosed a slow and irreversible inhibition of human MAO-B. Overall, the results support the suitability of the 4-triazolylalkyl propargylamine scaffold for exploring the design of multipotent anti-Alzheimer compounds endowed with irreversible MAO-B inhibitory activity.
[Mh] Termos MeSH primário: Desenho de Drogas
Inibidores da Monoaminoxidase/farmacologia
Monoaminoxidase/metabolismo
Pargilina/farmacologia
[Mh] Termos MeSH secundário: Relação Dose-Resposta a Droga
Seres Humanos
Simulação de Acoplamento Molecular
Estrutura Molecular
Inibidores da Monoaminoxidase/química
Pargilina/análogos & derivados
Pargilina/síntese química
Pargilina/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Monoamine Oxidase Inhibitors); 9MV14S8G3E (Pargyline); EC 1.4.3.4 (Monoamine Oxidase)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170910
[Lr] Data última revisão:
170910
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160712
[St] Status:MEDLINE


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[PMID]:27226189
[Au] Autor:Tammimaki A; Aonurm-Helm A; Kaenmaki M; Mannisto PT
[Ad] Endereço:Division of Pharmacology and Pharmacotherapy, Faculty of Pharmacy, University of Helsinki, Finland. anne.tammimaki@gmail.com.
[Ti] Título:Elimination of extracellular dopamine in the medial prefrontal cortex of conscious mice analysed using selective enzyme and uptake inhibitors.
[So] Source:J Physiol Pharmacol;67(2):301-9, 2016 Apr.
[Is] ISSN:1899-1505
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:We have shown in a previous study that in the medial prefrontal cortex (mPFC) of Comt knockout animals, uptake1 followed by oxidation accounts for approximately 50% and uptake2 followed by O-methylation for the remaining 50% of dopamine clearance. However, compensatory mechanisms in genetically modified animals may have affected the result. Therefore, in the present study, we gave a high dose (30 mg/kg) of tolcapone in combination with pargyline and reboxetine to C57BL/6J mice to see whether the earlier findings could be confirmed. The three drugs were also given together. We used intracerebral microdialysis to determine the levels of extracellular dopamine and its metabolites in the mPFC. In addition, we analyzed dopamine, 3,4-dihydroxyphenyl acetic acid (DOPAC) and homovanillic acid (HVA) contents in cortical and striatal synaptosomes to estimate the amount of releasable dopamine and dopamine turnover. In the prefrontal cortex of male C57BL/6J mice, the combination of two drugs (pargyline + tolcapone or reboxetine + tolcapone) generally elevated extracellular dopamine levels more than any single drug. Similar responses, although much weaker, were observed in female mice. Unexpectedly, triple treatment with pargyline, reboxetine and tolcapone did not increase dopamine outflow in the mPFC in either sex, and the treatment actually diminished dopamine outflow in the dorsal striatum. This seems to indicate that such an extensive treatment induces a fast and effective shut-down of dopamine release both in the mPFC and striatum to protect the brain from excess dopaminergic stimulation. The observed decrease in extracellular dopamine levels was not due to the depletion of releasable dopamine because abundant amounts of dopamine were present in synaptosomes. These results imply that the relative proportion of COMT-induced dopamine clearance may be somewhat lower than earlier estimated.
[Mh] Termos MeSH primário: Dopamina/metabolismo
Córtex Pré-Frontal/metabolismo
[Mh] Termos MeSH secundário: Ácido 3,4-Di-Hidroxifenilacético/metabolismo
Inibidores da Captação Adrenérgica/farmacologia
Animais
Benzofenonas/farmacologia
Catecol O-Metiltransferase/genética
Inibidores de Catecol O-Metiltransferase/farmacologia
Feminino
Ácido Homovanílico/metabolismo
Masculino
Camundongos Endogâmicos C57BL
Camundongos Knockout
Inibidores da Monoaminoxidase/farmacologia
Morfolinas/farmacologia
Nitrofenóis/farmacologia
Pargilina/farmacologia
Córtex Pré-Frontal/efeitos dos fármacos
Sinaptossomos/efeitos dos fármacos
Sinaptossomos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic Uptake Inhibitors); 0 (Benzophenones); 0 (Catechol O-Methyltransferase Inhibitors); 0 (Monoamine Oxidase Inhibitors); 0 (Morpholines); 0 (Nitrophenols); 102-32-9 (3,4-Dihydroxyphenylacetic Acid); 947S0YZ36I (reboxetine); 9MV14S8G3E (Pargyline); CIF6334OLY (tolcapone); EC 2.1.1.6 (Catechol O-Methyltransferase); VTD58H1Z2X (Dopamine); X77S6GMS36 (Homovanillic Acid)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170505
[Lr] Data última revisão:
170505
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160527
[St] Status:MEDLINE


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[PMID]:27160849
[Au] Autor:Zamoner LO; Aragão-Leoneti V; Mantoani SP; Rugen MD; Nepogodiev SA; Field RA; Carvalho I
[Ad] Endereço:School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Av. do Café s/n, Monte Alegre, Ribeirão Preto 14040-930, Brazil.
[Ti] Título:CuAAC click chemistry with N-propargyl 1,5-dideoxy-1,5-imino-D-gulitol and N-propargyl 1,6-dideoxy-1,6-imino-D-mannitol provides access to triazole-linked piperidine and azepane pseudo-disaccharide iminosugars displaying glycosidase inhibitory properties.
[So] Source:Carbohydr Res;429:29-37, 2016 Jun 24.
[Is] ISSN:1873-426X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Protecting group-free synthesis of 1,2:5,6-di-anhydro-D-mannitol, followed by ring opening with propargylamine and subsequent ring closure produced a separable mix of piperidine N-propargyl 1,5-dideoxy-1,5-imino-D-gulitol and azepane N-propargyl 1,6-dideoxy-1,6-imino-D-mannitol. In O-acetylated form, these two building blocks were subjected to CuAAC click chemistry with a panel of three differently azide-substituted glucose building blocks, producing iminosugar pseudo-disaccharides in good yield. The overall panel of eight compounds, plus 1-deoxynojirimycin (DNJ) as a benchmark, was evaluated as prospective inhibitors of almond ß-glucosidase, yeast α-glucosidase and barley ß-amylase. The iminosugar pseudo-disaccharides showed no inhibitory activity against almond ß-glucosidase, while the parent N-propargyl 1,5-dideoxy-1,5-imino-D-gulitol and N-propargyl 1,6-dideoxy-1,6-imino-D-mannitol likewise proved to be inactive against yeast α-glucosidase. Inhibitory activity could be reinstated in the former series by appropriate substitution on nitrogen. The greater activity of the piperidine could be rationalized based on docking studies. Further, potent inhibition of ß-amylase was observed with compounds from both the piperidine and azepane series.
[Mh] Termos MeSH primário: Inibidores Enzimáticos/síntese química
Compostos Heterocíclicos com 1 Anel/síntese química
Imino Açúcares/síntese química
Piperidinas/síntese química
Triazóis/síntese química
alfa-Glucosidases/química
beta-Amilase/química
beta-Glucosidase/química
[Mh] Termos MeSH secundário: 1-Desoxinojirimicina/química
Azidas/química
Química Click/métodos
Dissacarídeos/química
Inibidores Enzimáticos/química
Glucose/química
Compostos Heterocíclicos com 1 Anel/química
Hordeum/química
Hordeum/enzimologia
Imino Açúcares/química
Manitol/química
Pargilina/análogos & derivados
Pargilina/química
Piperidinas/química
Propilaminas/química
Prunus dulcis/química
Prunus dulcis/enzimologia
Saccharomyces cerevisiae/química
Saccharomyces cerevisiae/enzimologia
Triazóis/química
beta-Amilase/antagonistas & inibidores
beta-Glucosidase/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Azides); 0 (Disaccharides); 0 (Enzyme Inhibitors); 0 (Heterocyclic Compounds, 1-Ring); 0 (Imino Sugars); 0 (Piperidines); 0 (Propylamines); 0 (Triazoles); 19130-96-2 (1-Deoxynojirimycin); 2450-71-7 (propargylamine); 3OWL53L36A (Mannitol); 9MV14S8G3E (Pargyline); EC 3.2.1.2 (beta-Amylase); EC 3.2.1.20 (alpha-Glucosidases); EC 3.2.1.21 (beta-Glucosidase); IY9XDZ35W2 (Glucose)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:170119
[Lr] Data última revisão:
170119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160511
[St] Status:MEDLINE


  9 / 2564 MEDLINE  
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[PMID]:27031993
[Au] Autor:Watanabe K; Li J; Veerasamy N; Ghosh A; Carter RG
[Ad] Endereço:Department of Chemistry, Oregon State University , 153 Gilbert Hall, Corvallis, Oregon 97331, United States.
[Ti] Título:Stereoselective, Ag-Catalyzed Cyclizations To Access Polysubstituted Pyran Ring Systems: Synthesis of C1-C12 Subunit of Madeirolide A.
[So] Source:Org Lett;18(8):1744-7, 2016 Apr 15.
[Is] ISSN:1523-7052
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The exploration into the scope of a silver-catalyzed cyclization (AgCC) of propargyl benzoates for accessing pyran ring systems has been reported. The impact of the degree of substitution, nature of the substitution on the carbon backbone/benzoate moiety, and stereochemistry has been evaluated. The application of this methodology to the synthesis of the C1-C12 southern fragment of madeirolide A is disclosed.
[Mh] Termos MeSH primário: Benzoatos/química
Macrolídeos/síntese química
Pargilina/química
Piranos/química
Prata/química
[Mh] Termos MeSH secundário: Catálise
Ciclização
Macrolídeos/química
Estrutura Molecular
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Benzoates); 0 (Macrolides); 0 (Pyrans); 0 (madeirolide A); 3M4G523W1G (Silver); 9MV14S8G3E (Pargyline)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:160415
[Lr] Data última revisão:
160415
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160401
[St] Status:MEDLINE
[do] DOI:10.1021/acs.orglett.6b00414


  10 / 2564 MEDLINE  
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[PMID]:26936415
[Au] Autor:Demmer CS; Benoit E; Evano G
[Ad] Endereço:Laboratoire de Chimie Organique, Service de Chimie et PhysicoChimie Organiques, Université libre de Bruxelles (ULB) , Avenue F. D. Roosevelt 50, CP160/06, 1050 Brussels, Belgium.
[Ti] Título:Synthesis of Allenamides by Copper-Catalyzed Coupling of Propargylic Bromides and Nitrogen Nucleophiles.
[So] Source:Org Lett;18(6):1438-41, 2016 Mar 18.
[Is] ISSN:1523-7052
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:An efficient and general synthesis of allenamides derived from oxazolidinones and hydantoins is reported. Upon activation with a combination of a copper catalyst and a 2,2'-bipyridine derivative in the presence of an inorganic base, propargylic bromides were found to be suitable reagents for the direct allenylation of nitrogen nucleophiles by a formal copper-catalyzed S(N)2' reaction. Besides the availability of the starting materials, notable features of this route to allenamides are its mild reaction conditions, the reaction being performed at room temperature in most cases, and its applicability to the preparation of mono-, di-, as well as trisubstituted allenamides.
[Mh] Termos MeSH primário: Amidas/síntese química
Cobre/química
Nitrogênio/química
Oxazolidinonas/química
Pargilina/análogos & derivados
[Mh] Termos MeSH secundário: 2,2'-Dipiridil/química
Amidas/química
Catálise
Estrutura Molecular
Pargilina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amides); 0 (Oxazolidinones); 551W113ZEP (2,2'-Dipyridyl); 789U1901C5 (Copper); 9MV14S8G3E (Pargyline); F3H7ZXK9ZU (propargyl bromide); N762921K75 (Nitrogen)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160304
[St] Status:MEDLINE
[do] DOI:10.1021/acs.orglett.6b00372



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