Base de dados : MEDLINE
Pesquisa : D02.241 [Categoria DeCS]
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  1 / 11956 MEDLINE  
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[PMID]:29478648
[Au] Autor:Tella AC; Owalude SO; Olatunji SJ; Adimula VO; Elaigwu SE; Alimi LO; Ajibade PA; Oluwafemi OS
[Ad] Endereço:Department of Chemistry, University of Ilorin, P.M.B.1515 Ilorin, Nigeria. Electronic address: ac_tella@yahoo.co.uk.
[Ti] Título:Synthesis of zinc-carboxylate metal-organic frameworks for the removal of emerging drug contaminant (amodiaquine) from aqueous solution.
[So] Source:J Environ Sci (China);64:264-275, 2018 Feb.
[Is] ISSN:1001-0742
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:We herein report the removal of amodiaquine, an emerging drug contaminant from aqueous solution using [Zn (fum) (bpy)] and [Zn O(bdc) ] (fum=fumaric acid; bpy=4,4-bipyridine; bdc=benzene-1,4-dicarboxylate) metal-organic frameworks (MOFs) as adsorbents. The adsorbents were characterized by elemental analysis, Fourier transform infrared (FT-IR) spectroscopy, and powder X-ray diffraction (PXRD). Adsorption process for both adsorbents were found to follow the pseudo-first-order kinetics, and the adsorption equilibrium data fitted best into the Freundlich isotherm with the R values of 0.973 and 0.993 obtained for [Zn (fum) (bpy)] and [Zn O(bdc) ] respectively. The maximum adsorption capacities foramodiaquine in this study were found to be 0.478 and 47.62mg/g on the [Zn (fum) (bpy)] and [Zn O(bdc) ] MOFs respectively, and were obtained at pH of 4.3 for both adsorbents. FT-IR spectroscopy analysis of the MOFs after the adsorption process showed the presence of the drug. The results of the study showed that the prepared MOFs could be used for the removal of amodiaquine from wastewater.
[Mh] Termos MeSH primário: Amodiaquina/análise
Estruturas Metalorgânicas/química
Eliminação de Resíduos Líquidos/métodos
Poluentes Químicos da Água/análise
[Mh] Termos MeSH secundário: Adsorção
Amodiaquina/química
Ácidos Carboxílicos/química
Águas Residuais/química
Poluentes Químicos da Água/química
Difração de Raios X
Zinco/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carboxylic Acids); 0 (Metal-Organic Frameworks); 0 (Waste Water); 0 (Water Pollutants, Chemical); 220236ED28 (Amodiaquine); J41CSQ7QDS (Zinc)
[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:180227
[St] Status:MEDLINE


  2 / 11956 MEDLINE  
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[PMID]:29478638
[Au] Autor:Jin P; Song J; Wang XC; Jin X
[Ad] Endereço:School of Environmental and Municipal Engineering, Xi'an University of Architecture and Technology, Xi'an 710055, China. Electronic address: pkjin@xauat.edu.cn.
[Ti] Título:Two-dimensional correlation spectroscopic analysis on the interaction between humic acids and aluminum coagulant.
[So] Source:J Environ Sci (China);64:181-189, 2018 Feb.
[Is] ISSN:1001-0742
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In this study, two-dimensional correlation spectroscopy integrated with synchronous fluorescence and infrared absorption spectroscopy was employed to investigate the interaction between humic acids and aluminum coagulant at slightly acidic and neutral pH. Higher fluorescence quenching was produced for fulvic-like and humic-like fractions at pH5. At pH5, the humic-like fractions originating from the carboxylic acid, carboxyl and polysaccharide compounds were bound to aluminum first, followed by the fulvic-like fractions originating from the carboxyl and polysaccharide compounds. This finding also demonstrated that the activated functional groups of HA were involved in forming the Al-HA complex, which was accompanied by the removal of other groups by co-precipitation. Meanwhile, at pH7, almost no fluorescence quenching occurred, and surface complexation was observed to occur, in which the activated functional groups were absorbed on the amorphous Al(OH) . Two-dimensional FT-IR correlation spectroscopy indicated the sequence of HA structural change during coagulation with aluminum, with IR bands affected in the order of COOH>COO >NH deformation of amide II>aliphatic hydroxyl COH at pH5, and COO >aliphatic hydroxyl COH at pH7. This study provides a promising pathway for analysis and insight into the priority of functional groups in the interaction between organic matters and metal coagulants.
[Mh] Termos MeSH primário: Alumínio/química
Substâncias Húmicas
Modelos Químicos
[Mh] Termos MeSH secundário: Amidas
Dióxido de Carbono
Ácidos Carboxílicos
Fluorescência
Concentração de Íons de Hidrogênio
Radical Hidroxila
Espectrofotometria Infravermelho
Espectroscopia de Infravermelho com Transformada de Fourier
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amides); 0 (Carboxylic Acids); 0 (Humic Substances); 142M471B3J (Carbon Dioxide); 14485-07-5 (carboxyl radical); 3352-57-6 (Hydroxyl Radical); CPD4NFA903 (Aluminum)
[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:180227
[St] Status:MEDLINE


  3 / 11956 MEDLINE  
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[PMID]:29186227
[Au] Autor:Rodriguez-Muñiz GM; Gomez-Mendoza M; Nuin E; Andreu I; Marin ML; Miranda MA
[Ad] Endereço:Instituto Universitario Mixto de Tecnología Química (UPV-CSIC) Universitat Politècnica de València, Avda de los Naranjos s/n, 46022 Valencia, Spain.
[Ti] Título:"Snorkelling" vs. "diving" in mixed micelles probed by means of a molecular bathymeter.
[So] Source:Org Biomol Chem;15(48):10281-10288, 2017 Dec 13.
[Is] ISSN:1477-0539
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A photoactive bathymeter based on a carboxylic acid moiety covalently linked to a signalling methoxynaphthalene (MNP) fluorophore has been designed to prove the concept of "snorkelling" vs. "diving" in mixed micelles (MM). The carboxylic acid "floats" on the MM surface, while the MNP unit sinks deep in MM. The rate constants of MNP fluorescence quenching by iodide, which remains basically in water, consistently decrease with increasing spacer length, revealing different regions. This is associated with the distance MNP should "dive" in MM to achieve protection from aqueous reactants. Unequivocal proof of the exergonic photoinduced electron transfer was obtained from the UV-visible spectral signature of I upon steady-state photolysis. The applicability of the bathymeter was examined upon testing a family of MNP derivatives. The obtained results were validated by comparison with different lipophilicity tests: (i) a modified version of the K partition coefficient and (ii) the retention factor on thin layer chromatography. This concept could potentially be extended to test drugs or pharmacophores exhibiting any photoactive moiety.
[Mh] Termos MeSH primário: Ácidos Carboxílicos/química
Corantes Fluorescentes/química
Naftalenos/química
[Mh] Termos MeSH secundário: Micelas
Estrutura Molecular
Processos Fotoquímicos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carboxylic Acids); 0 (Fluorescent Dyes); 0 (Micelles); 0 (Naphthalenes)
[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:171130
[St] Status:MEDLINE
[do] DOI:10.1039/c7ob02595e


  4 / 11956 MEDLINE  
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[PMID]:28468238
[Au] Autor:Oka S; Kanagawa M; Doi Y; Schuster DM; Goodman MM; Yoshimura H
[Ad] Endereço:Research Center, Nihon Medi-Physics Co., Ltd., 3-1 Kitasode, Sodegaura, Chiba 299-0266, Japan. shuntaro_oka@nmp.co.jp.
[Ti] Título:Fasting Enhances the Contrast of Bone Metastatic Lesions in F-Fluciclovine-PET: Preclinical Study Using a Rat Model of Mixed Osteolytic/Osteoblastic Bone Metastases.
[So] Source:Int J Mol Sci;18(5), 2017 Apr 29.
[Is] ISSN:1422-0067
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:F-fluciclovine ( -1-amino-3- F-fluorocyclobutanecarboxylic acid) is an amino acid positron emission tomography (PET) tracer used for cancer staging (e.g., prostate and breast). Patients scheduled to undergo amino acid-PET are usually required to fast before PET tracer administration. However, there have been no reports addressing whether fasting improves fluciclovine-PET imaging. In this study, the authors investigated the influence of fasting on fluciclovine-PET using triple-tracer autoradiography with C-fluciclovine, [5,6-³H]-2-fluoro-2-deoxy-d-glucose (³H-FDG), and Tc-hydroxymethylene diphosphonate ( Tc-HMDP) in a rat breast cancer model of mixed osteolytic/osteoblastic bone metastases in which the animals fasted overnight. Lesion accumulation of each tracer was evaluated using the target-to-background (muscle) ratio. The mean ratios of C-fluciclovine in osteolytic lesions were 4.6 ± 0.8 and 2.8 ± 0.6, respectively, with and without fasting, while those for ³H-FDG were 6.9 ± 2.5 and 5.1 ± 2.0, respectively. In the peri-tumor bone formation regions (osteoblastic), where Tc-HMDP accumulated, the ratios of C-fluciclovine were 4.3 ± 1.4 and 2.4 ± 0.7, respectively, and those of ³H-FDG were 6.2 ± 3.8 and 3.3 ± 2.2, respectively, with and without fasting. These results suggest that fasting before F-fluciclovine-PET improves the contrast between osteolytic and osteoblastic bone metastatic lesions and background, as well as F-FDG-PET.
[Mh] Termos MeSH primário: Neoplasias Ósseas/diagnóstico por imagem
Neoplasias Ósseas/secundário
Osso e Ossos/diagnóstico por imagem
Ácidos Carboxílicos/análise
Meios de Contraste/análise
Ciclobutanos/análise
Tomografia por Emissão de Pósitrons/métodos
[Mh] Termos MeSH secundário: Animais
Neoplasias da Mama/diagnóstico por imagem
Linhagem Celular Tumoral
Jejum
Feminino
Fluordesoxiglucose F18/análise
Masculino
Ratos
Ratos Sprague-Dawley
Medronato de Tecnécio Tc 99m/análogos & derivados
Medronato de Tecnécio Tc 99m/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carboxylic Acids); 0 (Contrast Media); 0 (Cyclobutanes); 0Z5B2CJX4D (Fluorodeoxyglucose F18); 38R1Q0L1ZE (fluciclovine F-18); 72945-61-0 (technetium Tc 99m hydroxymethylene diphosphonate); X89XV46R07 (Technetium Tc 99m Medronate)
[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:170505
[St] Status:MEDLINE


  5 / 11956 MEDLINE  
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[PMID]:29311505
[Au] Autor:Tamura S; Sato K; Kawano T
[Ad] Endereço:Department of Medicinal and Organic Chemistry, School of Pharmacy, Iwate Medical University.
[Ti] Título:N-Alkylation Using Sodium Triacetoxyborohydride with Carboxylic Acids as Alkyl Sources.
[So] Source:Chem Pharm Bull (Tokyo);66(1):101-103, 2018.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:A versatile N-alkylation was performed using sodium triacetoxyborohydride and carboxylic acid as an alkyl source. The combination of these reagents furnished products different from those given previously by a similar reaction. Moreover, the mild conditions of our method allowed some functional groups to remain through the reaction, whereas they would react and be converted into other moieties in the similar reductive N-alkylation reported previously. Herein, we provide a new procedure for the preparation of various compounds containing nitrogen atoms.
[Mh] Termos MeSH primário: Aminas/síntese química
Boroidretos/química
Ácidos Carboxílicos/química
[Mh] Termos MeSH secundário: Alquilação
Aminas/química
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Borohydrides); 0 (Carboxylic Acids)
[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.c17-00716


  6 / 11956 MEDLINE  
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[PMID]:28458361
[Au] Autor:Nagano T; Nagano K; Nabeshi H; Yoshida T; Kamada H; Tsunoda SI; Gao JQ; Higashisaka K; Yoshioka Y; Tsutsumi Y
[Ad] Endereço:Laboratory of Toxicology and Safety Science, Graduate School of Pharmaceutical Sciences, Osaka University.
[Ti] Título:Modifying the Surface of Silica Nanoparticles with Amino or Carboxyl Groups Decreases Their Cytotoxicity to Parenchymal Hepatocytes.
[So] Source:Biol Pharm Bull;40(5):726-728, 2017.
[Is] ISSN:1347-5215
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:We previously reported that unmodified silica nanoparticles with diameters of 70 nm (nSP70) induced liver damage in mice, whereas nSP70 modified with carboxyl or amino groups did not. In addition, we have found that both unmodified and modified nSP70s localize in both Kupffer cells and parenchymal hepatocytes. We therefore evaluated the contributions of nSP70 uptake by these cell populations to liver damage. To this end, we pretreated mice with gadolinium (III) chloride hydrate (GdCl ) to prevent nSP70 uptake by Kupffer cells, subsequently injected the mice with either type of nSP70, and then assessed plasma levels of alanine aminotransferase (ALT). In mice given GdCl , unmodified nSP70 increased ALT levels. From these data, we hypothesized that in GdCl -treated mice, the unmodified nSP70 that was prevented from entering Kupffer cells was shunted to parenchymal hepatocytes, where it induced cytotoxicity and increased liver damage. In contrast, GdCl pretreatment had no effect on ALT levels in mice injected with surface-modified nSP70s, suggesting that modified nSP70s spared parenchymal hepatocytes and thus induced negligible liver damage. In cytotoxicity analyses, the viability of a parenchymal hepatocyte line was greater when exposed to surface-modified nSP70s than to unmodified nSP70s. These findings imply that the decreased liver damage associated with surface-modified compared with unmodified nSP70 is attributable to decreased cytotoxicity to parenchymal hepatocytes.
[Mh] Termos MeSH primário: Aminas/química
Ácidos Carboxílicos/química
Nanopartículas/química
Dióxido de Silício/química
[Mh] Termos MeSH secundário: Alanina Transaminase/análise
Animais
Linhagem Celular
Sobrevivência Celular/efeitos dos fármacos
Doença Hepática Induzida por Substâncias e Drogas/enzimologia
Doença Hepática Induzida por Substâncias e Drogas/patologia
Feminino
Gadolínio/química
Hepatócitos/efeitos dos fármacos
Macrófagos do Fígado/efeitos dos fármacos
Testes de Função Hepática
Camundongos
Camundongos Endogâmicos BALB C
Nanopartículas/toxicidade
Tamanho da Partícula
Dióxido de Silício/toxicidade
Propriedades de Superfície
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Carboxylic Acids); 7631-86-9 (Silicon Dioxide); AU0V1LM3JT (Gadolinium); EC 2.6.1.2 (Alanine Transaminase); P7082WY76D (gadolinium chloride)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180212
[Lr] Data última revisão:
180212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE
[do] DOI:10.1248/bpb.b16-00917


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[PMID]:28462837
[Au] Autor:Khadtare N; Stephani R; Korlipara V
[Ad] Endereço:Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY 11439, United States.
[Ti] Título:Design, synthesis and evaluation of 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acid derivatives as ET receptor selective antagonists using FRET assay.
[So] Source:Bioorg Med Chem Lett;27(11):2281-2285, 2017 06 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The endothelin axis and in particular the two receptor subtypes, ET and ET , are under investigation for the treatment of various diseases such as pulmonary arterial hypertension, fibrosis, renal failure and cancer. Previous work in our lab has shown that 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acid derivatives exhibit noteworthy endothelin receptor antagonist activity. A series of analogues with modifications centered around position 6 of the heterocyclic quinolone core and replacement of the aryl carboxylic acid group with an isosteric tetrazole ring was designed and synthesized to further optimize the structure activity relationship. The endothelin receptor antagonist activity was determined by in vitro Förster resonance energy transfer (FRET) using GeneBLAzer® assay technology. The most potent member of this series exhibited ET receptor antagonist activity in the subnanomolar range with an IC value of 0.8nM, and was 1000-fold selective for the ET receptor compared to the ET receptor. Its activity and selectivity profile resembles that of the most recently approved drug, macitentan.
[Mh] Termos MeSH primário: Ácidos Carboxílicos/química
Ácidos Carboxílicos/farmacologia
Quinolinas/química
Quinolinas/farmacologia
Receptor de Endotelina A/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Ácidos Carboxílicos/síntese química
Antagonistas dos Receptores de Endotelina/síntese química
Antagonistas dos Receptores de Endotelina/química
Antagonistas dos Receptores de Endotelina/farmacologia
Transferência Ressonante de Energia de Fluorescência
Seres Humanos
Concentração Inibidora 50
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (1,4-dihydroquinoline); 0 (Carboxylic Acids); 0 (Endothelin Receptor Antagonists); 0 (Quinolines); 0 (Receptor, Endothelin A)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE


  8 / 11956 MEDLINE  
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[PMID]:28918097
[Au] Autor:Li J; Wu F; Liu X; Zou Y; Chen H; Li Z; Zhang L
[Ad] Endereço:School of Bioscience and Bioengineering, South China University of Technology, Guangzhou 510006, PR China.
[Ti] Título:Synthesis and bioevaluation of 1-phenyl-pyrazole-4-carboxylic acid derivatives as potent xanthine oxidoreductase inhibitors.
[So] Source:Eur J Med Chem;140:20-30, 2017 Nov 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A diverse library of 1-phenyl-pyrazole-4-carboxylic acid derivatives were synthesized and evaluated for their inhibitory potency against xanthine oxidoreductase (XOR) in vitro and vivo, and the structure-activity relationship (SAR) analyses were also presented. Approximately half of the target compounds exhibited the inhibitory potency for XOR at the nanomolar level. Compounds 16c, 16d, and 16f emerged as the most potent xanthine oxidoreductase inhibitors with IC values of 5.7, 5.7 and 4.2 nM, respectively, in comparison to febuxostat (IC of 5.4 nM). Steady-state kinetics measurements indicated that 16c is a mixed-type inhibitor. A computer molecular docking study of 16c bound to XOR was performed to gain an insight into its bind mode and SAR for the series. A potassium oxonate-hypoxanthine-induced hyperuricemia model in mice was chosen to further confirm the hypouricemic effects of 16c and 16f, and the results demonstrated that 16c exhibits similar hypouricemic potency to febuxostat.
[Mh] Termos MeSH primário: Ácidos Carboxílicos/farmacologia
Inibidores Enzimáticos/farmacologia
Pirazóis/farmacologia
Xantina Desidrogenase/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Ácidos Carboxílicos/síntese química
Ácidos Carboxílicos/química
Relação Dose-Resposta a Droga
Inibidores Enzimáticos/síntese química
Inibidores Enzimáticos/química
Hiperuricemia/induzido quimicamente
Hiperuricemia/tratamento farmacológico
Camundongos
Camundongos Endogâmicos ICR
Modelos Moleculares
Estrutura Molecular
Ácido Oxônico/administração & dosagem
Pirazóis/síntese química
Pirazóis/química
Relação Estrutura-Atividade
Xantina Desidrogenase/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carboxylic Acids); 0 (Enzyme Inhibitors); 0 (Pyrazoles); 4R7FFA00RX (potassium oxonate); 5VT6420TIG (Oxonic Acid); EC 1.17.1.4 (Xanthine Dehydrogenase)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171106
[Lr] Data última revisão:
171106
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170918
[St] Status:MEDLINE


  9 / 11956 MEDLINE  
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[PMID]:28873471
[Au] Autor:Rasse DP; Budai A; O'Toole A; Ma X; Rumpel C; Abiven S
[Ad] Endereço:Department of Soil Quality and Climate Change, Norwegian Institute of Bioeconomy Research, Ås, Norway.
[Ti] Título:Persistence in soil of Miscanthus biochar in laboratory and field conditions.
[So] Source:PLoS One;12(9):e0184383, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Evaluating biochars for their persistence in soil under field conditions is an important step towards their implementation for carbon sequestration. Current evaluations might be biased because the vast majority of studies are short-term laboratory incubations of biochars produced in laboratory-scale pyrolyzers. Here our objective was to investigate the stability of a biochar produced with a medium-scale pyrolyzer, first through laboratory characterization and stability tests and then through field experiment. We also aimed at relating properties of this medium-scale biochar to that of a laboratory-made biochar with the same feedstock. Biochars were made of Miscanthus biomass for isotopic C-tracing purposes and produced at temperatures between 600 and 700°C. The aromaticity and degree of condensation of aromatic rings of the medium-scale biochar was high, as was its resistance to chemical oxidation. In a 90-day laboratory incubation, cumulative mineralization was 0.1% for the medium-scale biochar vs. 45% for the Miscanthus feedstock, pointing to the absence of labile C pool in the biochar. These stability results were very close to those obtained for biochar produced at laboratory-scale, suggesting that upscaling from laboratory to medium-scale pyrolyzers had little effect on biochar stability. In the field, the medium-scale biochar applied at up to 25 t C ha-1 decomposed at an estimated 0.8% per year. In conclusion, our biochar scored high on stability indices in the laboratory and displayed a mean residence time > 100 years in the field, which is the threshold for permanent removal in C sequestration projects.
[Mh] Termos MeSH primário: Carvão Vegetal/análise
Laboratórios
Poaceae/química
[Mh] Termos MeSH secundário: Aerobiose
Benzeno/análise
Biomarcadores/análise
Carbono/análise
Dióxido de Carbono/análise
Ácidos Carboxílicos/análise
Compostos Orgânicos/análise
Análise de Componente Principal
Estações do Ano
Solo/química
Temperatura Ambiente
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers); 0 (Carboxylic Acids); 0 (Organic Chemicals); 0 (Soil); 0 (biochar); 142M471B3J (Carbon Dioxide); 16291-96-6 (Charcoal); 7440-44-0 (Carbon); J64922108F (Benzene)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170906
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0184383


  10 / 11956 MEDLINE  
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[PMID]:28857471
[Au] Autor:Pirali T; Ciraolo E; Aprile S; Massarotti A; Berndt A; Griglio A; Serafini M; Mercalli V; Landoni C; Campa CC; Margaria JP; Silva RL; Grosa G; Sorba G; Williams R; Hirsch E; Tron GC
[Ad] Endereço:Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale "A. Avogadro", Largo Donegani 2, 28100, Novara, Italy.
[Ti] Título:Identification of a Potent Phosphoinositide 3-Kinase Pan Inhibitor Displaying a Strategic Carboxylic Acid Group and Development of Its Prodrugs.
[So] Source:ChemMedChem;12(18):1542-1554, 2017 Sep 21.
[Is] ISSN:1860-7187
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Activation of the phosphoinositide 3-kinase (PI3K) pathway is a key signaling event in cancer, inflammation, and other proliferative diseases. PI3K inhibitors are already approved for some specific clinical indications, but their systemic on-target toxicity limits their larger use. In particular, whereas toxicity is tolerable in acute treatment of life-threatening diseases, this is less acceptable in chronic conditions. In the past, the strategy to overcome this drawback was to block selected isoforms mainly expressed in leukocytes, but redundancy within the PI3K family members challenges the effectiveness of this approach. On the other hand, decreasing exposure to selected target cells represents a so-far unexplored alternative to circumvent systemic toxicity. In this manuscript, we describe the generation of a library of triazolylquinolones and the development of the first prodrug pan-PI3K inhibitor.
[Mh] Termos MeSH primário: Ácidos Carboxílicos/química
Inibidores Enzimáticos/química
Fosfatidilinositol 3-Quinases/antagonistas & inibidores
Pró-Fármacos/química
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação
Ácidos Carboxílicos/metabolismo
Ácidos Carboxílicos/farmacologia
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Desenho de Drogas
Inibidores Enzimáticos/metabolismo
Inibidores Enzimáticos/farmacologia
Seres Humanos
Ligações de Hidrogênio
Concentração Inibidora 50
Camundongos
Microssomos/metabolismo
Simulação de Dinâmica Molecular
Fosfatidilinositol 3-Quinases/metabolismo
Pró-Fármacos/metabolismo
Pró-Fármacos/farmacologia
Ligação Proteica
Isoformas de Proteínas/antagonistas & inibidores
Isoformas de Proteínas/metabolismo
Quinolonas/química
Quinolonas/metabolismo
Quinolonas/farmacologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carboxylic Acids); 0 (Enzyme Inhibitors); 0 (Prodrugs); 0 (Protein Isoforms); 0 (Quinolones); EC 2.7.1.- (Phosphatidylinositol 3-Kinases)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171009
[Lr] Data última revisão:
171009
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170901
[St] Status:MEDLINE
[do] DOI:10.1002/cmdc.201700340



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