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Pesquisa : D02.455.326.271 [Categoria DeCS]
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[PMID]:29408856
[Au] Autor:Kimura-Suda H; Takahata M; Ito T; Shimizu T; Kanazawa K; Ota M; Iwasaki N
[Ad] Endereço:Graduate School of Photonics Science, Chitose Institute of Science and Technology, Chitose, Hokkaido, Japan.
[Ti] Título:Quick and easy sample preparation without resin embedding for the bone quality assessment of fresh calcified bone using fourier transform infrared imaging.
[So] Source:PLoS One;13(2):e0189650, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Fourier transform infrared (FTIR) imaging is a powerful tool for the assessment of bone quality; however, it requires the preparation of thin bone sections. Conventional poly(methyl methacrylate) (PMMA) embedding for the preparation of sections takes more than two weeks and causes denaturation of the bone. Development of a quick and easy sample preparation technique without denaturation is needed for accurate clinical evaluation of fresh calcified bone using FTIR imaging. Frozen sectioning allows the quick and easy preparation of thin sections without denaturation, but it requires a substrate with good chemical resistance and improved heat shock resistance. Polypropylene (PP) film afforded both good chemical resistance and greater heat shock resistance, and the 4-µm-thick PP film coated with glue was thin enough for the IR beam to pass through it, while the optical anisotropy of infrared bands overlapping with PO43- band was negligible. The bone quality of femoral thin sections prepared by the conventional PMMA embedding and sectioning procedure (RESIN-S) or the newly developed frozen sectioning procedure (FROZEN-S) was evaluated by FTIR imaging. The mineral-to-matrix ratio and crystallinity in the RESIN-S sections were higher than those in the FROZEN-S sections, whereas the carbonate-to-phosphate ratio in the RESIN-S sections was lower than that in the FROZEN-S sections. In RESIN-S, the increased mineral-to-matrix ratio could be caused by dehydration, and the increased crystallinity and decreased carbonate-to-phosphate ratio might be consequence of dissolution of bone mineral during PMMA embedding. Therefore, the combined use of PP film coated with glue and the frozen sectioning procedure without denaturation appears well suited to the assessment of the bone quality of fresh calcified bone using FTIR imaging.
[Mh] Termos MeSH primário: Osso e Ossos/diagnóstico por imagem
Calcificação Fisiológica
Espectroscopia de Infravermelho com Transformada de Fourier/métodos
[Mh] Termos MeSH secundário: Alcenos
Animais
Camundongos
Camundongos Endogâmicos BALB C
Polimetil Metacrilato
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Alkenes); 9011-14-7 (Polymethyl Methacrylate); AUG1H506LY (propylene)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180207
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0189650


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[PMID]:29386433
[Au] Autor:Hatakeyama S
[Ad] Endereço:Graduate School of Biomedical Sciences, Nagasaki University.
[Ti] Título:[Stereocontrolled Total Synthesis of Biologically Active Natural Products].
[So] Source:Yakugaku Zasshi;138(2):191-209, 2018.
[Is] ISSN:1347-5231
[Cp] País de publicação:Japan
[La] Idioma:jpn
[Ab] Resumo: This review article describes the total syntheses of englerin A, ophiodilactones A and B, marinomycin A, N-methylwelwitindolinone C isothiocyanate, tirandamycins A-D, and tirandalydigin, which possess intriguing biological activities and challenging structures with characteristic ring systems. The focus is on the synthetic methodologies that lead to the highly stereocontrolled assembly of these natural products.
[Mh] Termos MeSH primário: Produtos Biológicos/síntese química
[Mh] Termos MeSH secundário: Alcenos/síntese química
Alcenos/química
Aminoglicosídeos/síntese química
Aminoglicosídeos/química
Derivados de Benzeno/síntese química
Derivados de Benzeno/química
Produtos Biológicos/química
Alcaloides de Indol/síntese química
Alcaloides de Indol/química
Lactonas/síntese química
Lactonas/química
Macrolídeos/síntese química
Macrolídeos/química
Conformação Molecular
Sesquiterpenos de Guaiano/síntese química
Sesquiterpenos de Guaiano/química
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Alkenes); 0 (Aminoglycosides); 0 (Benzene Derivatives); 0 (Biological Products); 0 (Indole Alkaloids); 0 (Lactones); 0 (Macrolides); 0 (N-methylwelwitindolinone B isothiocyanate); 0 (Sesquiterpenes, Guaiane); 0 (englerin A); 0 (marinomycin A); 0 (ophiodilactone A); 0 (ophiodilactone B); 0 (tirandamycin C); 0 (tirandamycin D); 114118-91-1 (tirandalydigin); 34429-70-4 (tirandamycin A); 60587-14-6 (tirandamycin B)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180228
[Lr] Data última revisão:
180228
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180202
[St] Status:MEDLINE
[do] DOI:10.1248/yakushi.17-00187


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[PMID]:29253825
[Au] Autor:Schinkel L; Lehner S; Knobloch M; Lienemann P; Bogdal C; McNeill K; Heeb NV
[Ad] Endereço:Empa, Swiss Federal Laboratories for Materials Testing and Research, Laboratory for Advanced Analytical Technologies, Überlandstrasse 129, CH-8600 Dübendorf, Switzerland; ETH, Swiss Federal Institute of Technology, Institute of Biogeochemistry and Pollutant Dynamic, Universitätsstrasse 16, CH-8092 Z
[Ti] Título:Transformation of chlorinated paraffins to olefins during metal work and thermal exposure - Deconvolution of mass spectra and kinetics.
[So] Source:Chemosphere;194:803-811, 2018 Mar.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Chlorinated paraffins (CPs) are high production volume chemicals widely used as additives in metal working fluids. Thereby, CPs are exposed to hot metal surfaces which may induce degradation processes. We hypothesized that the elimination of hydrochloric acid would transform CPs into chlorinated olefins (COs). Mass spectrometry is widely used to detect CPs, mostly in the selected ion monitoring mode (SIM) evaluating 2-3 ions at mass resolutions R < 20'000. This approach is not suited to detected COs, because their mass spectra strongly overlap with CPs. We applied a mathematical deconvolution method based on full-scan MS data to separate interfered CP/CO spectra. Metal drilling indeed induced HCl-losses. CO proportions in exposed mixtures of chlorotridecanes increased. Thermal exposure of chlorotridecanes at 160, 180, 200 and 220 °C also induced dehydrohalogenation reactions and CO proportions also increased. Deconvolution of respective mass spectra is needed to study the CP transformation kinetics without bias from CO interferences. Apparent first-order rate constants (k ) increased up to 0.17, 0.29 and 0.46 h for penta-, hexa- and heptachloro-tridecanes exposed at 220 °C. Respective half-life times (τ ) decreased from 4.0 to 2.4 and 1.5 h. Thus, higher chlorinated paraffins degrade faster than lower chlorinated ones. In conclusion, exposure of CPs during metal drilling and thermal treatment induced HCl losses and CO formation. It is expected that CPs and COs are co-released from such processes. Full-scan mass spectra and subsequent deconvolution of interfered signals is a promising approach to tackle the CP/CO problem, in case of insufficient mass resolution.
[Mh] Termos MeSH primário: Alcenos/síntese química
Hidrocarbonetos Clorados/química
Parafina/química
[Mh] Termos MeSH secundário: Monitoramento Ambiental/métodos
Temperatura Alta
Hidrocarbonetos Clorados/análise
Cinética
Espectrometria de Massas/métodos
Metalurgia
Parafina/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkenes); 0 (Hydrocarbons, Chlorinated); 8002-74-2 (Paraffin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180228
[Lr] Data última revisão:
180228
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171219
[St] Status:MEDLINE


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[PMID]:29394011
[Au] Autor:Saladino R; Chiocchini U; Botta G; Delfino M; Conigliaro R; Mosesso P
[Ti] Título:Free radical scavenging capacity and protective effect of natural substances in peloids from the thermal spring pool Bagnaccio (Viterbo, Italy).
[So] Source:J Cosmet Sci;67(2):71-92, 2016 Mar-Apr.
[Is] ISSN:1525-7886
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Natural peloids from sulfurous thermal springs are largely used in cosmetic and pelotherapy for the treatment of different dermatological conditions, including skin aging, dermatitis, and other eczemas. The beneficial effects are correlated to mineralogical and other thermal properties, as well as to the presence of natural substances with specific antioxidant activity. Few data are available for the comparison between natural peloids and synthetic (i.e., artificially maturated) muds. In this context, the natural substances and antioxidant activity of natural white mud (WM) and dark mud (DM) peloids from the sulfurous thermal spring pool Bagnaccio (Viterbo, Italy) have been studied in detail to evaluate possible relationships between physicochemical properties and therapeutic effect. A large panel of natural substances in WM and DM were characterized for the first time by ³¹P-nuclear magnetic resonance and gas chromatography associated to mass spectrometry analysis. Polar fractions of WM and DM peloids were characterized by the presence of several bioactive natural compounds, showing high antioxidant activity and DNA protective effect, as evaluated by 2,2-diphenyl-1-picrylhydrazyl assay, and hydrogen peroxide­induced DNA breakage in the alkaline comet assay. The antioxidant activity and DNA protective effect could be attributed to radical scavenging rather than a modulatory effect on the induced DNA repair, and are of order of intensity higher than that reported for synthetic muds.
[Mh] Termos MeSH primário: Alcaloides/farmacologia
Depuradores de Radicais Livres/farmacologia
Hidrocarbonetos Aromáticos/farmacologia
Fenóis/farmacologia
Terpenos/farmacologia
[Mh] Termos MeSH secundário: Alcaloides/química
Alcaloides/isolamento & purificação
Alcanos/química
Alcanos/isolamento & purificação
Alcanos/farmacologia
Alcenos/química
Alcenos/isolamento & purificação
Alcenos/farmacologia
Animais
Compostos de Bifenilo/antagonistas & inibidores
Compostos de Bifenilo/química
Células CHO
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Ensaio Cometa
Cricetulus
DNA/efeitos dos fármacos
Depuradores de Radicais Livres/química
Depuradores de Radicais Livres/isolamento & purificação
Fontes Termais
Seres Humanos
Hidrocarbonetos Aromáticos/química
Hidrocarbonetos Aromáticos/isolamento & purificação
Peróxido de Hidrogênio/antagonistas & inibidores
Peróxido de Hidrogênio/química
Itália
Espectroscopia de Ressonância Magnética
Camundongos
Terapia por Lama
Fenóis/química
Fenóis/isolamento & purificação
Picratos/antagonistas & inibidores
Picratos/química
Terpenos/química
Terpenos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Alkanes); 0 (Alkenes); 0 (Biphenyl Compounds); 0 (Free Radical Scavengers); 0 (Hydrocarbons, Aromatic); 0 (Phenols); 0 (Picrates); 0 (Terpenes); 9007-49-2 (DNA); BBX060AN9V (Hydrogen Peroxide); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180222
[Lr] Data última revisão:
180222
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180203
[St] Status:MEDLINE


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[PMID]:29342183
[Au] Autor:Nixon LJ; Morrison WR; Rice KB; Brockerhoff EG; Leskey TC; Guzman F; Khrimian A; Goldson S; Rostás M
[Ad] Endereço:Bio-Protection Research Centre, Lincoln University, Lincoln, Canterbury, New Zealand.
[Ti] Título:Identification of volatiles released by diapausing brown marmorated stink bug, Halyomorpha halys (Hemiptera: Pentatomidae).
[So] Source:PLoS One;13(1):e0191223, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The brown marmorated stink bug, Halyomorpha halys, is an agricultural and urban pest that has become widely established as an invasive species of major concern in the USA and across Europe. This species forms large aggregations when entering diapause, and it is often these aggregations that are found by officials conducting inspections of internationally shipped freight. Identifying the presence of diapausing aggregations of H. halys using their emissions of volatile organic compounds (VOCs) may be a potential means for detecting and intercepting them during international freight inspections. Headspace samples were collected from aggregations of diapausing H. halys using volatile collection traps (VCTs) and solid phase microextraction. The only compound detected in all samples was tridecane, with small amounts of (E)-2-decenal found in most samples. We also monitored the release of defensive odors, following mechanical agitation of diapausing and diapause-disrupted adult H. halys. Diapausing groups were significantly more likely to release defensive odors than diapause-disrupted groups. The predominant compounds consistently found from both groups were tridecane, (E)-2-decenal, and 4-oxo-(E)-2-hexenal, with a small abundance of dodecane. Our findings show that diapausing H. halys do release defensive compounds, and suggest that volatile sampling may be feasible to detect H. halys in freight.
[Mh] Termos MeSH primário: Heterópteros/química
Odorantes/análise
Compostos Orgânicos Voláteis/química
[Mh] Termos MeSH secundário: Aldeídos/análise
Alcanos/análise
Alcenos/análise
Animais
Diapausa
Cromatografia Gasosa-Espectrometria de Massas
Heterópteros/crescimento & desenvolvimento
Heterópteros/fisiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 ((2E)-decenal); 0 (4-oxo-(E)-2-hexenal); 0 (Aldehydes); 0 (Alkanes); 0 (Alkenes); 0 (Volatile Organic Compounds); 11A386X1QH (n-dodecane); A3LZF0L939 (tridecane)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180221
[Lr] Data última revisão:
180221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180118
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0191223


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[PMID]:29311504
[Au] Autor:Konishi H
[Ad] Endereço:School of Pharmaceutical Sciences, University of Shizuoka.
[Ti] Título:Creation of Novel Toxic Gas Surrogates and the Development of Safe and Facile Catalytic Reactions.
[So] Source:Chem Pharm Bull (Tokyo);66(1):1-19, 2018.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The use of toxic gas surrogates in organic reactions instead of the gas itself contributes to enhancing the safety, practicality, and efficiency of the reactions involved. Our efforts toward the creation of toxic gas surrogates and the development of a series of catalytic reactions using these surrogates are described. Improvements in substrate scope during the hydroesterification of alkenes using formates facilitated by the Ru-imidazole catalyst system provided the opportunity to discover that phenyl formate is a useful carbon monoxide (CO) surrogate for the generation of CO and phenol under weakly basic conditions. This discovery triggered the development of highly reactive but stable CO surrogates and a variety of Pd-catalyzed carbonylative transformations. N-Formylsaccharin facilitated the use of additional nucleophiles in carbonylation reactions that provided access to a variety of carbonyl compounds. Detailed experimental and theoretical mechanistic studies into the generation of CO from phenyl formate suggest that CO generation proceeds via a concerted E2 α-elimination. Furthermore, a known surrogate of sulfur dioxide was applied for the first time to the selective syntheses of cyclic sulfonamides and sulfinamides, confirming that the surrogate operates as an "S=O" source. Notably, the reactions described herein are scalable and can be performed without the use of external toxic gases and specialized reaction vessels; they are easy and simple to perform and demonstrate enormous potential for industrial application.
[Mh] Termos MeSH primário: Alcenos/química
Monóxido de Carbono/química
Ésteres/síntese química
Paládio/química
[Mh] Termos MeSH secundário: Catálise
Ésteres/química
Estrutura Molecular
Fenóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Alkenes); 0 (Esters); 0 (Phenols); 5TWQ1V240M (Palladium); 7U1EE4V452 (Carbon Monoxide)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180213
[Lr] Data última revisão:
180213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180110
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c17-00795


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[PMID]:29256506
[Au] Autor:Lee J; Radomkit S; Torker S; Del Pozo J; Hoveyda AH
[Ad] Endereço:Department of Chemistry, Merkert Chemistry Center, Boston College, Chestnut Hill, Massachusetts 02467, USA.
[Ti] Título:Mechanism-based enhancement of scope and enantioselectivity for reactions involving a copper-substituted stereogenic carbon centre.
[So] Source:Nat Chem;10(1):99-108, 2018 01.
[Is] ISSN:1755-4349
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A rapidly emerging set of catalytic reactions involves intermediates that contain a copper-substituted stereogenic carbon centre. Here, we demonstrate that an intimate understanding of this distinction provides ways for addressing limitations in reaction scope and explaining why unexpected variations in enantioselectivity often occur. By using catalytic enantioselective Cu-boryl addition to alkenes as the model process, we elucidate several key mechanistic principles. We show that higher electrophile concentration can lead to elevated enantioselectivity. This is because diastereoselective Cu-H elimination may be avoided and/or achiral Cu-boryl intermediates can be converted to allyl-B(pin) rather than add to an alkene. We illustrate that lower alkene amounts and/or higher chiral ligand concentration can minimize the deleterious influence of achiral Cu-alkyl species, resulting in improved enantiomeric ratios. Moreover, and surprisingly, we find that enantioselectivities are higher with the less reactive allylphenyl carbonates as chemoselective copper-hydride elimination is faster with an achiral Cu-alkyl species.
[Mh] Termos MeSH primário: Alcenos/química
Compostos de Boro/química
Cobre/química
Compostos Organometálicos/química
[Mh] Termos MeSH secundário: Catálise
Técnicas de Química Sintética
Modelos Químicos
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Alkenes); 0 (Boron Compounds); 0 (Organometallic Compounds); 789U1901C5 (Copper)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180123
[Lr] Data última revisão:
180123
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171220
[St] Status:MEDLINE
[do] DOI:10.1038/nchem.2861


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[PMID]:28464524
[Au] Autor:Démolis A; Eternot M; Essayem N; Rataboul F
[Ad] Endereço:CNRS, UMR 5256, IRCELYON, Institut de recherches sur la catalyse et l'environnement de Lyon, Université Lyon 1, 2 avenue Albert Einstein, F-, 69626, Villeurbanne, France.
[Ti] Título:New Insights into the Reactivity of Biomass with Butenes for the Synthesis of Butyl Levulinates.
[So] Source:ChemSusChem;10(12):2612-2617, 2017 06 22.
[Is] ISSN:1864-564X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:This article reports a detailed study on the reactivity of levulinic acid and cellulose with 1-butene and iso-butene for the catalytic formation of sec- and tert-butyl levulinates. The influence of catalyst type and various solvent conditions have been investigated to assess the potential of a sustainable transformation. A very simple and efficient procedure was discovered by using reusable Amberlyst-15 in the absence of solvent to form, from levulinic acid and iso-butene, tert-butyl levulinate (70 % yield), a compound very difficult to prepare by other means. sec-Butyl levulinate (66 % yield) was obtained by using Amberlyst-15 in γ-butyrolactone as a biosourced solvent. The original procedure was also extended notably by directly using cellulose as a reactant. In the presence of a catalytic amount of H SO , it was possible to form sec-butyl levulinate (19 % yield) from 1-butene in a more efficient way than by using the alcohol as an esterifying agent.
[Mh] Termos MeSH primário: Alcenos/química
Biomassa
Ácidos Levulínicos/química
Ácidos Levulínicos/síntese química
[Mh] Termos MeSH secundário: Catálise
Celulose/química
Técnicas de Química Sintética
Solventes/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Alkenes); 0 (Levulinic Acids); 0 (Solvents); 25167-67-3 (butylene); 9004-34-6 (Cellulose); RYX5QG61EI (levulinic acid)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:180118
[Lr] Data última revisão:
180118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.1002/cssc.201700416


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[PMID]:29199223
[Au] Autor:Hirashima SI; Narushima T; Kawada M; Nakashima K; Hanai K; Koseki Y; Miura T
[Ad] Endereço:Tokyo University of Pharmacy and Life Sciences.
[Ti] Título:Asymmetric Conjugate Additions of Carbonyl Compounds to Nitroalkenes under Solvent-Free Conditions Using Fluorous Diaminomethylenemalononitrile Organocatalyst.
[So] Source:Chem Pharm Bull (Tokyo);65(12):1185-1190, 2017.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:The novel fluorous organocatalyst bearing a diaminomethylenemalononitrile motif is prepared. The fluorous organocatalyst efficiently promotes asymmetric conjugate additions of ketones to nitroalkenes and results in high yields of these addition products with excellent enantioselectivities under solvent-free conditions.
[Mh] Termos MeSH primário: Alcenos/química
Cetonas/química
Nitrilos/química
[Mh] Termos MeSH secundário: Catálise
Nitrocompostos/química
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkenes); 0 (Ketones); 0 (Nitriles); 0 (Nitro Compounds); EBL1KKS93J (dicyanmethane)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180110
[Lr] Data última revisão:
180110
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171205
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c17-00596


  10 / 8402 MEDLINE  
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[PMID]:29232578
[Au] Autor:Lopes SMM; Novais JS; Costa DCS; Castro HC; Figueiredo AMS; Ferreira VF; Pinho E Melo TMVD; da Silva FC
[Ad] Endereço:CQC and Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal.
[Ti] Título:Hetero-Diels-Alder reactions of novel 3-triazolyl-nitrosoalkenes as an approach to functionalized 1,2,3-triazoles with antibacterial profile.
[So] Source:Eur J Med Chem;143:1010-1020, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:The generation and reactivity of 3-triazolyl-nitrosoalkenes are reported for the first time. The study showed that hetero-Diels-Alder reaction of these heterodienes is an interesting synthetic strategy to functionalized 1,2,3-triazoles, including 1,2,3-triazolyl-pyrroles, 1,2,3-triazolyl-dipyrromethanes and 1,2,3-triazolyl-indoles. The evaluation of the antibacterial profile against Gram-positive and Gram-negative strains revealed the new 5,5'-diethyldipyrromethane bearing a side chain incorporating a triazole and oxime moieties. The antibacterial profile detected was within the Clinical and Laboratory Standard Institute (CLSI) range and against important Staphylococcus species including Methicillin-resistant strain (S. aureus ATCC 25923, S. epidermidis ATCC 12228 and S. simulans ATCC 27851 and MRSA). Interestingly, this new 1,2,3-triazole presented hemocompatibility and low in silico toxicity profile similar to antibiotics current in use. It also has an usual antibiofilm activity against MRSA, which reinforced its potential as a new antibacterial prototype.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Staphylococcus/efeitos dos fármacos
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Alcenos/química
Antibacterianos/síntese química
Antibacterianos/química
Biofilmes/efeitos dos fármacos
Reação de Cicloadição
Relação Dose-Resposta a Droga
Testes de Sensibilidade Microbiana
Estrutura Molecular
Compostos Nitrosos/química
Staphylococcus/crescimento & desenvolvimento
Relação Estrutura-Atividade
Triazóis/síntese química
Triazóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkenes); 0 (Anti-Bacterial Agents); 0 (Nitroso Compounds); 0 (Triazoles)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171213
[St] Status:MEDLINE



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