Base de dados : MEDLINE
Pesquisa : E05.197 [Categoria DeCS]
Referências encontradas : 4034 [refinar]
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[PMID]:28450244
[Au] Autor:El-Naggar AWM; Senna MM; Mostafa TA; Helal RH
[Ad] Endereço:Radiation Chemistry Department, National Center for Radiation Research and Technology, Nasr City, Atomic Energy Authority, Cairo, Egypt. Electronic address: ab_nagga@yahoo.com.
[Ti] Título:Radiation synthesis and drug delivery properties of interpenetrating networks (IPNs) based on poly(vinyl alcohol)/ methylcellulose blend hydrogels.
[So] Source:Int J Biol Macromol;102:1045-1051, 2017 Sep.
[Is] ISSN:1879-0003
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Gamma radiation was used to prepare blend hydrogels from poly(vinyl alcohol) (PVA) and low ratios of methylcellulose (MC). The structure-property behavior was characterized by IR spectroscopy, gel fraction, differential scanning calorimetry (DSC) and swelling at room temperature and different pH values. The PVA/MC hydrogels were used as a carrier for doxycycline hyclate (DOX-h) drug. The results showed that the gel fraction of PVA/MC hydrogels decreased greatly with increasing the ratio of MC in the initial feeding solution. The PVA/MC hydrogels displayed pH-sensitive swelling character. The drug uptake-release study indicated that PVA/MC hydrogels possessed controlled release behavior and that the release process depends on pH. In this respect, the release of DOX-h drug was significant in alkaline medium.
[Mh] Termos MeSH primário: Portadores de Fármacos/química
Portadores de Fármacos/síntese química
Hidrogéis/química
Hidrogéis/síntese química
Metilcelulose/química
Álcool de Polivinil/química
[Mh] Termos MeSH secundário: Técnicas de Química Sintética
Doxiciclina/química
Liberação Controlada de Fármacos
Raios gama
Concentração de Íons de Hidrogênio
Radioquímica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Hydrogels); 9002-89-5 (Polyvinyl Alcohol); 9004-67-5 (Methylcellulose); N12000U13O (Doxycycline)
[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:170429
[St] Status:MEDLINE


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[PMID]:29339755
[Au] Autor:Rout SK; Friedmann MP; Riek R; Greenwald J
[Ad] Endereço:Laboratory of Physical Chemistry, ETH Zürich, Vladimir-Prelog-Weg 2, 8093, Zürich, Switzerland.
[Ti] Título:A prebiotic template-directed peptide synthesis based on amyloids.
[So] Source:Nat Commun;9(1):234, 2018 01 16.
[Is] ISSN:2041-1723
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The prebiotic replication of information-coding molecules is a central problem concerning life's origins. Here, we report that amyloids composed of short peptides can direct the sequence-selective, regioselective and stereoselective condensation of amino acids. The addition of activated DL-arginine and DL-phenylalanine to the peptide RFRFR-NH in the presence of the complementary template peptide Ac-FEFEFEFE-NH yields the isotactic product FRFRFRFR-NH , 1 of 64 possible triple addition products, under conditions in which the absence of template yields only single and double additions of mixed stereochemistry. The templating mechanism appears to be general in that a different amyloid formed by (Orn)V(Orn)V(Orn)V(Orn)V-NH and Ac-VDVDVDVDV-NH is regioselective and stereoselective for N-terminal, L-amino-acid addition while the ornithine-valine peptide alone yields predominantly sidechain condensation products with little stereoselectivity. Furthermore, the templating reaction is stable over a wide range of pH (5.6-8.6), salt concentration (0-4 M NaCl), and temperature (25-90 °C), making the amyloid an attractive model for a prebiotic peptide replicating system.
[Mh] Termos MeSH primário: Aminoácidos/química
Amiloide/química
Técnicas de Química Sintética/métodos
Peptídeos/química
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Aminoácidos/genética
Aminoácidos/metabolismo
Amiloide/metabolismo
Amiloide/ultraestrutura
Arginina/química
Arginina/genética
Arginina/metabolismo
Concentração de Íons de Hidrogênio
Microscopia Eletrônica
Origem da Vida
Biossíntese Peptídica/genética
Peptídeos/genética
Peptídeos/metabolismo
Fenilalanina/química
Fenilalanina/genética
Fenilalanina/metabolismo
Cloreto de Sódio/química
Estereoisomerismo
Temperatura Ambiente
Moldes Genéticos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amino Acids); 0 (Amyloid); 0 (Peptides); 451W47IQ8X (Sodium Chloride); 47E5O17Y3R (Phenylalanine); 94ZLA3W45F (Arginine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180118
[St] Status:MEDLINE
[do] DOI:10.1038/s41467-017-02742-3


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[PMID]:28511560
[Au] Autor:Li W; Xiao Y
[Ad] Endereço:a School of Chemical and Environmental Engineering , Hanshan Normal University , Chaozhou , P.R. China.
[Ti] Título:Synthesis and in vitro antitumour activities of lupeol derivatives.
[So] Source:Nat Prod Res;32(1):48-53, 2018 Jan.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Nine lupeol derivatives were synthesised and assayed in vitro for their antitumour activities against three human tumour cells lines, A549, LAC and HepG2. Of lupeol derivaties, six were new compounds, and five compounds against A549 cells, four compounds against HepG2 cells and three compounds against LAC cells were effective in reducing viability, and the most promising compounds 5, 6 and 9 exhibited high activities against lung and liver cancer cells, even higher activities than those of adriamycin.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Triterpenos Pentacíclicos/química
[Mh] Termos MeSH secundário: Células A549
Antineoplásicos/síntese química
Linhagem Celular Tumoral
Técnicas de Química Sintética
Ensaios de Seleção de Medicamentos Antitumorais
Células Hep G2
Seres Humanos
Concentração Inibidora 50
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Pentacyclic Triterpenes); O268W13H3O (lupeol)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170518
[St] Status:MEDLINE
[do] DOI:10.1080/14786419.2017.1329729


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[PMID]:29379007
[Au] Autor:Ye CX; Melcamu YY; Li HH; Cheng JT; Zhang TT; Ruan YP; Zheng X; Lu X; Huang PQ
[Ad] Endereço:Department of Chemistry and Fujian Provincial Key Laboratory of Chemical Biology, College of Chemistry and Chemical Engineering, Xiamen University, Xiamen, Fujian, 361005, China.
[Ti] Título:Dual catalysis for enantioselective convergent synthesis of enantiopure vicinal amino alcohols.
[So] Source:Nat Commun;9(1):410, 2018 01 29.
[Is] ISSN:2041-1723
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Enantiopure vicinal amino alcohols and derivatives are essential structural motifs in natural products and pharmaceutically active molecules, and serve as main chiral sources in asymmetric synthesis. Currently known asymmetric catalytic protocols for this class of compounds are still rare and often suffer from limited scope of substrates, relatively low regio- or stereoselectivities, thus prompting the development of more effective methodologies. Herein we report a dual catalytic strategy for the convergent enantioselective synthesis of vicinal amino alcohols. The method features a radical-type Zimmerman-Traxler transition state formed from a rare earth metal with a nitrone and an aromatic ketyl radical in the presence of chiral N,N'-dioxide ligands. In addition to high level of enantio- and diastereoselectivities, our synthetic protocol affords advantages of simple operation, mild conditions, high-yielding, and a broad scope of substrates. Furthermore, this protocol has been successfully applied to the concise synthesis of pharmaceutically valuable compounds (e.g., ephedrine and selegiline).
[Mh] Termos MeSH primário: Aldeídos/química
Amino Álcoois/síntese química
Técnicas de Química Sintética
Ácidos de Lewis/química
Óxidos de Nitrogênio/química
[Mh] Termos MeSH secundário: Catálise
Luz
Oxirredução
Processos Fotoquímicos
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Aldehydes); 0 (Amino Alcohols); 0 (Lewis Acids); 0 (Nitrogen Oxides); 0 (nitrones)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180227
[Lr] Data última revisão:
180227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180131
[St] Status:MEDLINE
[do] DOI:10.1038/s41467-017-02698-4


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[PMID]:28741644
[Au] Autor:Bieszczad B; Gilheany DG
[Ad] Endereço:Centre for Synthesis and Chemical Biology, School of Chemistry, University College Dublin, Belfield, Dublin 4, Ireland. declan.gilheany@ucd.ie.
[Ti] Título:Highly stereoselective construction of the C2 stereocentre of α-tocopherol (vitamin E) by asymmetric addition of Grignard reagents to ketones.
[So] Source:Org Biomol Chem;15(31):6483-6492, 2017 Aug 09.
[Is] ISSN:1477-0539
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Tertiary alcohol precursors of both C2 diastereoisomers of α-tocopherol were prepared in three ways by our recently reported asymmetric Grignard synthesis. The versatility of Grignard chemistry inherent in its three-way disconnection was exploited to allow the synthesis of three product grades: 77 : 23 dr (5 steps), 81 : 19 dr (5 steps) and 96 : 4 dr (7 steps, one gram scale) from readily available and abundant starting materials. The products were converted to their respective α-tocopherols in 3 steps, which allowed a definitive re-assignment of their absolute configurations.
[Mh] Termos MeSH primário: Cetonas/química
Vitaminas/síntese química
alfa-Tocoferol/síntese química
[Mh] Termos MeSH secundário: Álcoois/síntese química
Álcoois/química
Técnicas de Química Sintética
Indicadores e Reagentes
Cetonas/síntese química
Conformação Molecular
Estereoisomerismo
Vitaminas/química
alfa-Tocoferol/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alcohols); 0 (Indicators and Reagents); 0 (Ketones); 0 (Vitamins); H4N855PNZ1 (alpha-Tocopherol)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170726
[St] Status:MEDLINE
[do] DOI:10.1039/c7ob00751e


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[PMID]:27779269
[Au] Autor:Liu Y; Zhou CJ; Li Q; Wang H
[Ad] Endereço:School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, 510006, China.
[Ti] Título:Total synthesis of (±)-ganocins B and C.
[So] Source:Org Biomol Chem;14(44):10362-10365, 2016 Nov 08.
[Is] ISSN:1477-0539
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The first total synthesis of structurally unique polycyclic phenolic meroterpenoids, ganocins B and C is reported. The synthesis features gold-catalyzed intramolecular cascade cyclization to construct the C/D ring bearing an angular methyl group, diastereoselective Michael addition, and acid-mediated one-pot Robinson cyclization/deprotection/isomerization.
[Mh] Termos MeSH primário: Terpenos/química
Terpenos/síntese química
[Mh] Termos MeSH secundário: Catálise
Técnicas de Química Sintética
Ciclização
Estereoisomerismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Terpenes)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180206
[Lr] Data última revisão:
180206
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161026
[St] Status:MEDLINE


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[PMID]:28456080
[Au] Autor:Tang C; Nie D; Tang G; Gao S; Liu S; Wen F; Tang X
[Ad] Endereço:Guangdong Engineering Research Center for Medical Radiopharmaceuticals Translational Application PET-CT Center and Department of Nuclear Medicine, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou 510080, China; Department of Nuclear Medicine, The Fifth Affiliated Hospital, Sun Yat-Se
[Ti] Título:Radiosynthesis and biological evaluation of N-(2-[ F]fluoropropionyl)-3,4-dihydroxy-l-phenylalanine as a PET tracer for oncologic imaging.
[So] Source:Nucl Med Biol;50:39-46, 2017 Jul.
[Is] ISSN:1872-9614
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: Several C and F labeled 3,4-dihydroxy-l-phenylalanine (l-DOPA) analogues have been used for neurologic and oncologic diseases, especially for brain tumors and neuroendocrine tumors PET imaging. However, F-labeled N-substituted l-DOPA analogues have not been reported so far. In the current study, radiosynthesis and biological evaluation of a new F-labeled l-DOPA analogue, N-(2-[ F]fluoropropionyl)-3,4-dihydroxy-l-phenylalanine ([ F]FPDOPA) for tumor PET imaging are performed. METHODS: The synthesis of [ F]FPDOPA was via a two-step reaction sequence from 4-nitrophenyl-2-[ F]fluoropropionate ([ F]NFP). The biodistribution of [ F]FPDOPA was determined in normal Kunming mice. In vitro competitive inhibition and protein incorporation experiments were performed with SPC-A-1 lung adenocarcinoma cell lines. PET/CT studies of [ F]FPDOPA were conducted in C6 rat glioma and SPC-A-1 human lung adenocarcinoma and H460 human large cell lung cancer-bearing nude mice. RESULTS: [ F]FPDOPA was prepared with a decay-corrected radiochemical yield of 28±5% and a specific activity of 50±15GBq/µmol (n=10) within 125min. In vitro cell experiments showed that [ F]FPDOPA uptake in SPC-A-1 cells was primarily transported through Na -independent system L, with Na -dependent system B and system ASC partly involved in it. Biodistribution data in mice showed that renal-bladder route was the main excretory system of [ F]FPDOPA. PET imaging demonstrated intense accumulation of [ F]FPDOPA in several tumor xenografts, with (8.50±0.40)%ID/g in C6 glioma, (6.30±0.12)%ID/g in SPC-A-1 lung adenocarcinoma, and (6.50±0.10)%ID/g in H460 large cell lung cancer, respectively. CONCLUSION: A novel N-substituted F-labeled L-DOPA analogue [ F]FPDOPA is synthesized and evaluated in vitro and in vivo. The results support that [ F]FPDOPA seems to be a potential PET tracer for tumor imaging, especially be a better potential PET tracer than [ F]fluoro-2-deoxy-d-glucose ([ F]FDG) for brain tumor imaging.
[Mh] Termos MeSH primário: Neoplasias/diagnóstico por imagem
Fenilalanina/análogos & derivados
Fenilalanina/síntese química
Fenilalanina/farmacocinética
Tomografia por Emissão de Pósitrons
[Mh] Termos MeSH secundário: Animais
Linhagem Celular Tumoral
Técnicas de Química Sintética
Estabilidade de Medicamentos
Seres Humanos
Camundongos
Neoplasias/metabolismo
Fenilalanina/química
Traçadores Radioativos
Radioquímica
Ratos
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Radioactive Tracers); 47E5O17Y3R (Phenylalanine)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180126
[Lr] Data última revisão:
180126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170430
[St] Status:MEDLINE


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[PMID]:28460347
[Au] Autor:Kumar R; Kumar M; Singh A; Singh N; Maity J; Prasad AK
[Ad] Endereço:Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi 110 007, India.
[Ti] Título:Synthesis of novel C-4'-spiro-oxetano-α-L-ribonucleosides.
[So] Source:Carbohydr Res;445:88-92, 2017 Jun 05.
[Is] ISSN:1873-426X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The synthesis of novel C-4'-spiro-oxetano-α-L-ribonucleosides T and U in 39 and 45% overall yields have been achieved from 2',3',5'-tri-O-acetyl-4'-C-p-toluenesulfonyloxymethyl-ß-D-xylofuranosylthymine and 2',3',5'-tri-O-acetyl-4'-C-p-toluenesulfonyloxymethyl-ß-D-xylofuranosyluracil, respectively. Both the tosylated nucleoside precursors have been synthesized following recently developed Novozyme -435 catalyzed methodology.
[Mh] Termos MeSH primário: Ribonucleosídeos/química
Ribonucleosídeos/síntese química
Compostos de Espiro/química
[Mh] Termos MeSH secundário: Técnicas de Química Sintética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ribonucleosides); 0 (Spiro Compounds)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180125
[Lr] Data última revisão:
180125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE


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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


  10 / 4034 MEDLINE  
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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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