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[PMID]:27778071
[Au] Autor:Kiesel BF; Parise RA; Guo J; Huryn DM; Johnston PA; Colombo R; Sen M; Grandis JR; Beumer JH; Eiseman JL
[Ad] Endereço:Cancer Therapeutics Program, The University of Pittsburgh Cancer Institute, Hillman Cancer Center, Room G27e, 5117 Centre Ave, Pittsburgh, PA, 15213, USA.
[Ti] Título:Toxicity, pharmacokinetics and metabolism of a novel inhibitor of IL-6-induced STAT3 activation.
[So] Source:Cancer Chemother Pharmacol;78(6):1225-1235, 2016 Dec.
[Is] ISSN:1432-0843
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:PURPOSE: The oncogenic transcription factor signal transducer and activator of transcription 3 (STAT3) promotes gene transcription involved in cancer, and its activation by IL-6 is found in head and neck squamous cell carcinoma. Four triazolothiadizine STAT3 pathway inhibitors were evaluated to prioritize a single compound for in vivo examination. METHODS: Metabolic stability in mouse liver microsome incubation was used to evaluate four triazolothiadizine analogues, and UPCDC-10205 was administered to mice IV as single or multiple doses to evaluate toxicity. Single-dose pharmacokinetics (PK), bioavailability and metabolism were studied after IV 4 mg/kg, PO 4 mg/kg, or PO 30 mg/kg suspension in 1% carboxymethyl cellulose. Mice were euthanized between 5 min to 24 h after dosing, and plasma and tissues were analyzed by LC-MS. Non-compartmental PK parameters were determined. RESULTS: Of the four triazolothiadizine analogues evaluated, UPCDC-10205 was metabolically most stable. The maximum soluble dose of 4 mg/kg in 10% Solutol™ was not toxic to mice after single and multiple doses. PK analysis showed extensive tissue distribution and rapid plasma clearance. Bioavailability was ~5%. A direct glucuronide conjugate was identified as the major metabolite which was recapitulated in vitro. CONCLUSIONS: Rapid clearance of UPCDC-10205 was thought to be the result of phase II metabolism despite its favorable stability in a phase I in vitro metabolic stability assay. The direct glucuronidation explains why microsomal stability (reflective of phase I metabolism) did not translate to in vivo metabolic stability. UPCDC-10205 did not demonstrate appropriate exposure to support efficacy studies in the current formulation.
[Mh] Termos MeSH primário: Interleucina-6/antagonistas & inibidores
Fator de Transcrição STAT3/antagonistas & inibidores
Tiadiazinas/farmacocinética
Triazóis/farmacocinética
[Mh] Termos MeSH secundário: Animais
Feminino
Camundongos
Microssomos Hepáticos/metabolismo
Tiadiazinas/toxicidade
Triazóis/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Interleukin-6); 0 (STAT3 Transcription Factor); 0 (Thiadiazines); 0 (Triazoles); 0 (UPCDC-10205)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171201
[Lr] Data última revisão:
171201
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161026
[St] Status:MEDLINE


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[PMID]:28793993
[Au] Autor:Tribler S; Brandt CF; Petersen AH; Petersen JH; Fuglsang KA; Staun M; Broebech P; Moser CE; Jeppesen PB
[Ad] Endereço:Departments of Medical Gastroenterology and siri.tribler@regionh.dk.
[Ti] Título:Taurolidine-citrate-heparin lock reduces catheter-related bloodstream infections in intestinal failure patients dependent on home parenteral support: a randomized, placebo-controlled trial.
[So] Source:Am J Clin Nutr;106(3):839-848, 2017 Sep.
[Is] ISSN:1938-3207
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In patients with intestinal failure who are receiving home parenteral support (HPS), catheter-related bloodstream infections (CRBSIs) inflict health impairment and high costs. This study investigates the efficacy and safety of the antimicrobial catheter lock solution, taurolidine-citrate-heparin, compared with heparin 100 IE/mL on CRBSI occurrence. Forty-one high-risk patients receiving HPS followed in a tertiary HPS unit were randomly assigned in a double-blinded, placebo-controlled trial. External, stratified randomization was performed according to age, sex, and prior CRBSI incidence. The prior CRBSI incidence in the study population was 2.4 episodes/1000 central venous catheter (CVC) days [95% Poisson confidence limits (CLs): 2.12, 2.71 episodes/1000 CVC days]. The maximum treatment period was 2 y or until occurrence of a CRBSI or right-censoring because of CVC removal. The exact permutation tests were used to calculate values for the log-rank tests. Twenty patients received the taurolidine-citrate-heparin lock and 21 received the heparin lock, with 9622 and 6956 treatment days, respectively. In the taurolidine-citrate-heparin arm, no CRBSIs occurred, whereas 7 CRBSIs occurred in the heparin arm, with an incidence of 1.0/1000 CVC days (95% Poisson CLs: 0.4, 2.07/1000 CVC days; 0.005). The CVC removal rates were 0.52/1000 CVC days (95% Poisson CLs: 0.17, 1.21/1000 CVC days) and 1.72/1000 CVC days (95% Poisson CLs: 0.89, 3.0/1000 CVC days) in the taurolidine-citrate-heparin and heparin arm, respectively, tending to prolong CVC survival in the taurolidine arm ( = 0.06). Costs per treatment year were lower in the taurolidine arm (€2348) than in the heparin arm (€6744) owing to fewer admission days related to treating CVC-related complications ( = 0.02). In patients with intestinal failure who are life dependent on HPS, the taurolidine-citrate-heparin catheter lock demonstrates a clinically substantial and cost-beneficial reduction of CRBSI occurrence in a high-risk population compared with heparin. This trial was registered at clinicaltrials.gov as NCT01948245.
[Mh] Termos MeSH primário: Bacteriemia/prevenção & controle
Infecções Relacionadas a Cateter/prevenção & controle
Cateteres Venosos Centrais/efeitos adversos
Citratos/uso terapêutico
Heparina/uso terapêutico
Enteropatias/terapia
Taurina/análogos & derivados
Tiadiazinas/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Idoso
Bacteriemia/epidemiologia
Infecções Relacionadas a Cateter/epidemiologia
Análise Custo-Benefício
Feminino
Seres Humanos
Incidência
Intestinos
Masculino
Meia-Idade
Nutrição Parenteral no Domicílio/métodos
Taurina/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Citrates); 0 (Thiadiazines); 1EQV5MLY3D (Taurine); 8OBZ1M4V3V (taurolidine); 9005-49-6 (Heparin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170919
[Lr] Data última revisão:
170919
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170811
[St] Status:MEDLINE
[do] DOI:10.3945/ajcn.117.158964


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[PMID]:28678857
[Au] Autor:Shevelev OB; Illarionova NB; Petrovski DV; Sarapultsev AP; Chupakhin ON; Moshkin MP
[Ad] Endereço:The federal research center Institute of Cytology and Genetics Siberian Branch of the Russian Academy of Sciences, Novosibirsk, Russia.
[Ti] Título:Effects of a compound from the group of substituted thiadiazines with hypothermia inducing properties on brain metabolism in rats, a study in vivo and in vitro.
[So] Source:PLoS One;12(7):e0180739, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The aim of the present study was to examine how administration of a compound of 1,3,4- thiadiazine class 2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide (L-17) with hypothermia inducing properties affects the brain metabolism. The mechanism by which L-17 induces hypothermia is unknown; it may involve hypothalamic central thermoregulation as well as act via inhibition of energy metabolism. We tested the hypothesis that L-17 may induce hypothermia by directly inhibiting energy metabolism. The study in vivo was carried out on Sprague-Dawley adult rats. Two doses of L-17 were administered (190 mg/kg and 760 mg/kg). Brain metabolites were analyzed in control and treated groups using magnetic resonance spectroscopy, along with blood flow rate measurements in carotid arteries and body temperature measurements. Further in vitro studies on primary cultures from rat hippocampus were carried out to perform a mitochondria function test of L-17 pre-incubation (100 µM, 30 min). Analysis of brain metabolites showed no significant changes in 190 mg/kg treated group along with a significant reduction in body temperature by 1.5°C. However, administration of L-17 in higher dose 760 mg/kg provoked changes in brain metabolites indicative of neurotoxicity as well as reduction in carotid arteries flow rate. In addition, a balance change of excitatory and inhibitory neurotransmitters was observed. The L-17 pre-incubation with cell primary cultures from rat brain showed no significant changes in mitochondrial function. The results obtained in the study indicate that acute administration of L-17 190 mg/kg in rats induces mild hypothermia with no adverse effects onto brain metabolism.
[Mh] Termos MeSH primário: Encéfalo/efeitos dos fármacos
Hipotermia Induzida
Tiadiazinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Temperatura Corporal
Encéfalo/metabolismo
Técnicas In Vitro
Angiografia por Ressonância Magnética
Espectroscopia de Ressonância Magnética
Masculino
Ratos
Ratos Sprague-Dawley
Tiadiazinas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Thiadiazines)
[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:170706
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0180739


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[PMID]:28595288
[Au] Autor:Li Y; Zhang Y; Liu X; Guo H
[Ad] Endereço:Department of Entomology, College of Plant Protection, Nanjing Agricultural University, Weigang No. 1, Nanjing, 210095, China.
[Ti] Título:Does Resistance to Buprofezin Improve Heat and Cold Tolerance of Laodelphax striatellus (Hemiptera: Delphacidae)?
[So] Source:Environ Entomol;46(4):988-994, 2017 08 01.
[Is] ISSN:1938-2936
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:There is ample evidence that insecticide resistance causes fitness costs and benefits in pests, while the impact of insecticide resistance on thermotolerance of pests is mostly unclear. The Laodelphax striatellus (Fallén), is an important rice insect pest, which has developed resistance to buprofezin in China. Here, we investigated differences in heat tolerance and cold tolerance among L. striatellus lines with variable buprofezin resistance. The lethal time for 50% of the individuals to die (LT50) at 40 °C increased with an increase in buprofezin resistance level, whereas both the survival rate under -22 °C and the supercooling point of planthoppers did not differ significantly between resistant and susceptible strains. The metabolic enzyme carboxylesterase was found to have an association with buprofezin resistance. Our research showed that buprofezin resistance was positively related with heat tolerance in L. striatellus, but it had no effect on cold tolerance. Insecticide resistance in L. striatellus may therefore have broader implications for the ecology of L. striatellus, and the management of buprofezin resistance in this pest may be challenging.
[Mh] Termos MeSH primário: Aclimatação
Resistência a Medicamentos/fisiologia
Hemípteros/fisiologia
Hormônios Juvenis/farmacologia
Tiadiazinas/farmacologia
[Mh] Termos MeSH secundário: Animais
Temperatura Baixa
Hemípteros/efeitos dos fármacos
Termotolerância
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Juvenile Hormones); 0 (Thiadiazines); 3B8KGI239I (buprofezin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171126
[Lr] Data última revisão:
171126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170609
[St] Status:MEDLINE
[do] DOI:10.1093/ee/nvx101


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[PMID]:28499168
[Au] Autor:Guerra A; Gonzalez-Naranjo P; Campillo NE; Varela J; Lavaggi ML; Merlino A; Cerecetto H; González M; Gomez-Barrio A; Escario JA; Fonseca-Berzal C; Yaluf G; Paniagua-Solis J; Páez JA
[Ad] Endereço:Instituto de Química Médica, Consejo Superior de Investigaciones Científicas (CSIC), Juan de la Cierva 3, 28006 Madrid, Spain.
[Ti] Título:Novel Imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides as antiproliferative trypanosoma cruzi drugs: Computational screening from neural network, synthesis and in vivo biological properties.
[So] Source:Eur J Med Chem;136:223-234, 2017 Aug 18.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A new family of imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxide with antiproliferative Trypanosoma cruzi properties was identified from a neural network model published by our group. The synthesis and evaluation of this new class of trypanocidal agents are described. These compounds inhibit the growth of Trypanosoma cruzi, comparable with benznidazole or nifurtimox. In vitro assays were performed to study their effects on the growth of the epimastigote form of the Tulahuen 2 strain, as well as the epimastigote and amastigote forms of CL clone B5 of Trypanosoma cruzi. To verify selectivity towards parasite cells, the non-specific cytotoxicity of the most relevant compounds was studied in mammalian cells, i.e. J774 murine macrophages and NCTC clone 929 fibroblasts. Furthermore, these compounds were assayed regarding the inhibition of cruzipain. In vivo studies revealed that one of the compounds, 19, showed interesting trypanocidal activity, and could be a very promising candidate for the treatment of Chagas disease.
[Mh] Termos MeSH primário: Imidazóis/farmacologia
Redes Neurais (Computação)
Tiadiazinas/farmacologia
Trypanosoma cruzi/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Proliferação Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Fibroblastos/efeitos dos fármacos
Imidazóis/síntese química
Imidazóis/química
Macrófagos/efeitos dos fármacos
Camundongos
Estrutura Molecular
Relação Estrutura-Atividade
Tiadiazinas/síntese química
Tiadiazinas/química
Trypanosoma cruzi/citologia
Trypanosoma cruzi/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Imidazoles); 0 (Thiadiazines); 0 (imidazo(4,5-c)(1,2,6)thiadiazine 2,2-dioxide)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170928
[Lr] Data última revisão:
170928
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170513
[St] Status:MEDLINE


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[PMID]:28365474
[Au] Autor:Ma XD; Hang LH; Shao DH; Shu WW; Hu XL; Luo H
[Ad] Endereço:Department of Anaesthesiology, Affiliated People's Hospital of Jiangsu University, Zhenjiang 212002, China.
[Ti] Título:TDAG8 activation attenuates cerebral ischaemia-reperfusion injury via Akt signalling in rats.
[So] Source:Exp Neurol;293:115-123, 2017 Jul.
[Is] ISSN:1090-2430
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: T-cell death-associated gene 8 (TDAG8), a member of the proton-sensitive G-protein-coupled receptor (GPCR) class with an immune-specific expression profile, was recently shown to be expressed in the rat brain; however, its role in ischaemic stroke remains unknown. METHODS: We initially confirmed the time-dependent expression of TDAG8 in rat brain tissue after ischaemic stroke and reperfusion. Further evaluations were performed to increase TDAG8 expression 6h prior to middle cerebral artery occlusion (MCAO) by injecting a specific agonist, BTB09089, into the lateral ventricle to increase TDAG8 expression. Twenty-four hours before MCAO, a specific small interfering RNA (siRNA) was introduced. The infarction volume, neurological deficit score and cleaved caspase-3 and Bcl-2 expression were used to assess the effects of TDAG8 on ischaemic stroke. Finally, the effects of TDAG8 on the development of primary cortical neurons exposed to oxygen-glucose deprivation (OGD) were investigated. RESULTS: TDAG8 expression increased both in vivo and in vitro. Pretreatment with BTB09089 up-regulated TDAG8 and Bcl-2 expression and down-regulated cleaved caspase-3 expression, while the infarction volume was reduced, and neurological deficits were ameliorated 24 and 72h after MCAO. However, the protective effects of TDAG8 were reversed when its level was reduced in TDAG8-deficient rats. More importantly, these findings are consistent with data from neurons subjected to OGD. CONCLUSIONS: TDAG8 plays an important neuroprotective role through inhibition of neuronal apoptosis and alleviation of neurological deficits by activating the Akt signalling pathway in rats.
[Mh] Termos MeSH primário: Isquemia Encefálica/metabolismo
Proteína Oncogênica v-akt/metabolismo
Receptores Acoplados a Proteínas-G/metabolismo
Traumatismo por Reperfusão/metabolismo
Transdução de Sinais/fisiologia
[Mh] Termos MeSH secundário: Animais
Isquemia Encefálica/complicações
Isquemia Encefálica/tratamento farmacológico
Células Cultivadas
Córtex Cerebral/citologia
Modelos Animais de Doenças
Embrião de Mamíferos
Regulação da Expressão Gênica/efeitos dos fármacos
Regulação da Expressão Gênica/fisiologia
Glucose/deficiência
Hipóxia/tratamento farmacológico
Hipóxia/metabolismo
L-Lactato Desidrogenase/metabolismo
Masculino
Doenças do Sistema Nervoso/tratamento farmacológico
Doenças do Sistema Nervoso/etiologia
Neurônios/efeitos dos fármacos
Fosfopiruvato Hidratase/metabolismo
Piridazinas/farmacologia
Piridazinas/uso terapêutico
RNA Interferente Pequeno/uso terapêutico
Ratos
Ratos Sprague-Dawley
Receptores Acoplados a Proteínas-G/genética
Traumatismo por Reperfusão/complicações
Traumatismo por Reperfusão/tratamento farmacológico
Transdução de Sinais/efeitos dos fármacos
Tiadiazinas/farmacologia
Tiadiazinas/uso terapêutico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3-((2,4-dichlorobenzyl)thio)-1,6-dimethyl-5,6-dihydro-1H-pyridazino(4,5-e)(1,3,4)thiadiazin-5-one); 0 (Pyridazines); 0 (RNA, Small Interfering); 0 (Receptors, G-Protein-Coupled); 0 (TDAG8 protein, rat); 0 (Thiadiazines); EC 1.1.1.27 (L-Lactate Dehydrogenase); EC 2.7.11.1 (Oncogene Protein v-akt); EC 4.2.1.11 (Phosphopyruvate Hydratase); IY9XDZ35W2 (Glucose)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170403
[St] Status:MEDLINE


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[PMID]:28248932
[Au] Autor:Mullard A
[Ti] Título:BACE inhibitor bust in Alzheimer trial.
[So] Source:Nat Rev Drug Discov;16(3):155, 2017 03 01.
[Is] ISSN:1474-1784
[Cp] País de publicação:England
[La] Idioma:eng
[Mh] Termos MeSH primário: Doença de Alzheimer/tratamento farmacológico
Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores
Ácido Aspártico Endopeptidases/antagonistas & inibidores
Óxidos S-Cíclicos
Tiadiazinas
[Mh] Termos MeSH secundário: Doença de Alzheimer/diagnóstico
Ensaios Clínicos como Assunto
Óxidos S-Cíclicos/administração & dosagem
Óxidos S-Cíclicos/efeitos adversos
Óxidos S-Cíclicos/uso terapêutico
Término Precoce de Ensaios Clínicos
Seres Humanos
Tiadiazinas/administração & dosagem
Tiadiazinas/efeitos adversos
Tiadiazinas/uso terapêutico
[Pt] Tipo de publicação:NEWS
[Nm] Nome de substância:
0 (Cyclic S-Oxides); 0 (Thiadiazines); 0 (verubecestat); EC 3.4.- (Amyloid Precursor Protein Secretases); EC 3.4.23.- (Aspartic Acid Endopeptidases); EC 3.4.23.46 (BACE1 protein, human)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170911
[Lr] Data última revisão:
170911
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170302
[St] Status:MEDLINE
[do] DOI:10.1038/nrd.2017.43


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[PMID]:28202490
[Au] Autor:Hawkes N
[Ad] Endereço:London.
[Ti] Título:Merck ends trial of potential Alzheimer's drug verubecestat.
[So] Source:BMJ;356:j845, 2017 Feb 15.
[Is] ISSN:1756-1833
[Cp] País de publicação:England
[La] Idioma:eng
[Mh] Termos MeSH primário: Doença de Alzheimer/tratamento farmacológico
Ensaios Clínicos como Assunto
Óxidos S-Cíclicos/uso terapêutico
Indústria Farmacêutica
Nootrópicos/uso terapêutico
Tiadiazinas/uso terapêutico
[Mh] Termos MeSH secundário: Doença de Alzheimer/líquido cefalorraquidiano
Amiloide/líquido cefalorraquidiano
Amiloide/efeitos dos fármacos
Anticorpos Monoclonais Humanizados/farmacologia
Anticorpos Monoclonais Humanizados/uso terapêutico
Óxidos S-Cíclicos/farmacologia
Indústria Farmacêutica/métodos
Seres Humanos
Nootrópicos/farmacologia
Índice de Gravidade de Doença
Tiadiazinas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amyloid); 0 (Antibodies, Monoclonal, Humanized); 0 (Cyclic S-Oxides); 0 (Nootropic Agents); 0 (Thiadiazines); 0 (verubecestat); 105J35OE21 (aducanumab)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170217
[St] Status:MEDLINE
[do] DOI:10.1136/bmj.j845


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[PMID]:27846059
[Au] Autor:Hulshof EC; Hanff LM; Olieman J; de Vette S; Driessen GJ; Meeussen C; Escher JC
[Ad] Endereço:From the *Department of Hospital Pharmacy, Erasmus MC, Sophia Children's Hospital, Rotterdam, the Netherlands; †Department of Dietetics, Erasmus MC, Sophia Children's Hospital, Rotterdam, the Netherlands; ‡Department of Paediatric Surgery, Erasmus MC, Sophia Children's Hospital, Rotterdam, the Netherlands; §Department of Infectious Disease and Immunology, Erasmus MC, Sophia Children's Hospital, Rotterdam, the Netherlands; and ¶Department of Paediatric Gastroenterology, Erasmus MC, Sophia Children's Hospital, Rotterdam, the Netherlands.
[Ti] Título:Taurolidine in Pediatric Home Parenteral Nutrition Patients.
[So] Source:Pediatr Infect Dis J;36(2):233-235, 2017 Feb.
[Is] ISSN:1532-0987
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:To reduce the incidence of catheter-related bloodstream infections in home parenteral nutrition patients, the use of taurolidine was introduced in the Sophia Children's Hospital in 2011. This introduction led to a reduction in catheter-related bloodstream infections: 12.7/1000 catheter days before the use of taurolidine, compared with 4.3/1000 catheter days afterwards (n = 7) [relative risk = 0.36, 95% confidence interval: 0.20-0.65 (P = 0.018)].
[Mh] Termos MeSH primário: Anti-Infecciosos/uso terapêutico
Bacteriemia
Infecções Relacionadas a Cateter
Nutrição Parenteral no Domicílio/estatística & dados numéricos
Taurina/análogos & derivados
Tiadiazinas/uso terapêutico
[Mh] Termos MeSH secundário: Anti-Infecciosos/administração & dosagem
Bacteriemia/tratamento farmacológico
Bacteriemia/epidemiologia
Bacteriemia/prevenção & controle
Infecções Relacionadas a Cateter/tratamento farmacológico
Infecções Relacionadas a Cateter/epidemiologia
Infecções Relacionadas a Cateter/prevenção & controle
Pré-Escolar
Seres Humanos
Lactente
Recém-Nascido
Nutrição Parenteral no Domicílio/efeitos adversos
Nutrição Parenteral no Domicílio/métodos
Estudos Retrospectivos
Taurina/administração & dosagem
Taurina/uso terapêutico
Tiadiazinas/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Thiadiazines); 1EQV5MLY3D (Taurine); 8OBZ1M4V3V (taurolidine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170622
[Lr] Data última revisão:
170622
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161116
[St] Status:MEDLINE
[do] DOI:10.1097/INF.0000000000001404


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Fotocópia
[PMID]:27933948
[Au] Autor:Scott JD; Li SW; Brunskill AP; Chen X; Cox K; Cumming JN; Forman M; Gilbert EJ; Hodgson RA; Hyde LA; Jiang Q; Iserloh U; Kazakevich I; Kuvelkar R; Mei H; Meredith J; Misiaszek J; Orth P; Rossiter LM; Slater M; Stone J; Strickland CO; Voigt JH; Wang G; Wang H; Wu Y; Greenlee WJ; Parker EM; Kennedy ME; Stamford AW
[Ti] Título:Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A ß-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease.
[So] Source:J Med Chem;59(23):10435-10450, 2016 Dec 08.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Verubecestat 3 (MK-8931), a diaryl amide-substituted 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative, is a high-affinity ß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor currently undergoing Phase 3 clinical evaluation for the treatment of mild to moderate and prodromal Alzheimer's disease. Although not selective over the closely related aspartyl protease BACE2, verubecestat has high selectivity for BACE1 over other key aspartyl proteases, notably cathepsin D, and profoundly lowers CSF and brain Aß levels in rats and nonhuman primates and CSF Aß levels in humans. In this annotation, we describe the discovery of 3, including design, validation, and selected SAR around the novel iminothiadiazinane dioxide core as well as aspects of its preclinical and Phase 1 clinical characterization.
[Mh] Termos MeSH primário: Doença de Alzheimer/tratamento farmacológico
Precursor de Proteína beta-Amiloide/antagonistas & inibidores
Óxidos S-Cíclicos/farmacologia
Descoberta de Drogas
Tiadiazinas/farmacologia
[Mh] Termos MeSH secundário: Doença de Alzheimer/metabolismo
Precursor de Proteína beta-Amiloide/metabolismo
Animais
Óxidos S-Cíclicos/síntese química
Óxidos S-Cíclicos/química
Cães
Relação Dose-Resposta a Droga
Seres Humanos
Macaca fascicularis
Modelos Moleculares
Estrutura Molecular
Ratos
Ratos Sprague-Dawley
Relação Estrutura-Atividade
Tiadiazinas/síntese química
Tiadiazinas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amyloid beta-Protein Precursor); 0 (Cyclic S-Oxides); 0 (Thiadiazines); 0 (verubecestat)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170615
[Lr] Data última revisão:
170615
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161210
[St] Status:MEDLINE



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