Base de dados : MEDLINE
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  1 / 1529 MEDLINE  
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[PMID]:29353671
[Au] Autor:Shimizu Y; Ishikawa M; Gotoh M; Fukasawa K; Yamamoto S; Iwasa K; Yoshikawa K; Murakami-Murofushi K
[Ad] Endereço:Endowed Research Division of Human Welfare Sciences, Ochanomizu University, Tokyo, Japan. Electronic address: y-shimuzu@lrc.or.jp.
[Ti] Título:Quantitative determination of cyclic phosphatidic acid and its carba analog in mouse organs and plasma using LC-MS/MS.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1076:15-21, 2018 Feb 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Cyclic phosphatidic acid (cPA), an analog of lysophosphatidic acid, is involved in the regulation of many cellular processes. A sensitive and specific method to quantify the molecular species of cPA is important for studying the physiological and pathophysiological roles of cPA. Here, we developed a liquid chromatography-tandem mass spectrometry (LC-MS/MS)-based quantification method for the simultaneous detection of cPA species having various fatty acids (16:0, 18:0, 18:1, and 18:2) as well as 2-carba-cPA, a chemically synthesized analog of cPA. Chromatography was performed using a reversed-phase C18 column. cPA species were detected using a triple quadrupole mass spectrometer. cPA 17:0 was used as an internal standard. Intra- and interday precision values (CV%) were within 10%. The linear range of detection for each cPA species was 0.01 µg/mL to 5 µg/mL, with correlation coefficients of 0.998 or higher. The developed method was applied to the quantification of cPA species in mouse plasma and organs. The concentrations of cPA 16:0, 18:0, and 18:1 were revealed to be significantly reduced in the brains of cuprizone-treated mice, a model of multiple sclerosis, compared with control mice. These findings could be important for understanding the roles of cPA in the neurodegenerative processes associated with multiple sclerosis.
[Mh] Termos MeSH primário: Compostos Heterocíclicos com 1 Anel/análise
Ácidos Fosfatídicos/análise
[Mh] Termos MeSH secundário: Animais
Cromatografia Líquida/métodos
Cuprizona/efeitos adversos
Compostos Heterocíclicos com 1 Anel/metabolismo
Limite de Detecção
Modelos Lineares
Masculino
Camundongos
Esclerose Múltipla/induzido quimicamente
Esclerose Múltipla/metabolismo
Especificidade de Órgãos
Ácidos Fosfatídicos/metabolismo
Reprodutibilidade dos Testes
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-carba-cyclic phosphatidic acid); 0 (Heterocyclic Compounds, 1-Ring); 0 (Phosphatidic Acids); 0 (cyclic phosphatidic acid 16:0); 5N16U7E0AO (Cuprizone)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180307
[Lr] Data última revisão:
180307
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180123
[St] Status:MEDLINE


  2 / 1529 MEDLINE  
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[PMID]:29286054
[Au] Autor:McCarthy MW; Walsh TJ
[Ad] Endereço:Weill Cornell Medical College, Department of Medicine, New York, New York, USA. mwm9004@med.cornell.edu.
[Ti] Título:Meropenem/vaborbactam fixed combination for the treatment of patients with complicated urinary tract infections.
[So] Source:Drugs Today (Barc);53(10):521-530, 2017 Oct.
[Is] ISSN:1699-3993
[Cp] País de publicação:Spain
[La] Idioma:eng
[Ab] Resumo:On August 29, 2017, the United States Food and Drug Administration (FDA) approved meropenem/ vaborbactam fixed combination for the treatment of adults with complicated urinary tract infections (cUTI). The decision was based on substantial preclinical and clinical data, including two recent trials involving hundreds of adults with cUTI. Meropenem/ vaborbactam represents a powerful new treatment option to address antibiotic-resistant pathogens, including Klebsiella pneumoniae carbapenemase-producing bacteria. In this paper, we examine the work that led to FDA approval, with special emphasis on molecular pharmacology, pharmacokinetics, metabolism, efficacy and drug safety. We also look ahead, to explore how this promising new antimicrobial agent might be used in the near future to confront other drug-resistant infections..
[Mh] Termos MeSH primário: Antibacterianos/uso terapêutico
Ácidos Borônicos/administração & dosagem
Compostos Heterocíclicos com 1 Anel/administração & dosagem
Tienamicinas/administração & dosagem
Infecções Urinárias/tratamento farmacológico
[Mh] Termos MeSH secundário: Ácidos Borônicos/efeitos adversos
Ácidos Borônicos/farmacocinética
Ácidos Borônicos/farmacologia
Ensaios Clínicos como Assunto
Interações Medicamentosas
Compostos Heterocíclicos com 1 Anel/efeitos adversos
Compostos Heterocíclicos com 1 Anel/farmacocinética
Compostos Heterocíclicos com 1 Anel/farmacologia
Seres Humanos
Tienamicinas/efeitos adversos
Tienamicinas/farmacocinética
Tienamicinas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Boronic Acids); 0 (Heterocyclic Compounds, 1-Ring); 0 (RPX7009); 0 (Thienamycins); FV9J3JU8B1 (meropenem)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180306
[Lr] Data última revisão:
180306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171230
[St] Status:MEDLINE
[do] DOI:10.1358/dot.2017.53.10.2721815


  3 / 1529 MEDLINE  
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[PMID]:28450564
[Au] Autor:Ahrens BJ; Li L; Ciminera AK; Chea J; Poku E; Bading JR; Weist MR; Miller MM; Colcher DM; Shively JE
[Ad] Endereço:Deparment of Molecular Immunology, Beckman Research Institute of the City of Hope, Duarte, California.
[Ti] Título:Diagnostic PET Imaging of Mammary Microcalcifications Using Cu-DOTA-Alendronate in a Rat Model of Breast Cancer.
[So] Source:J Nucl Med;58(9):1373-1379, 2017 Sep.
[Is] ISSN:1535-5667
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The development of improved breast cancer screening methods is hindered by a lack of cancer-specific imaging agents and effective small-animal models to test them. The purpose of this study was to evaluate Cu-DOTA-alendronate as a mammary microcalcification-targeting PET imaging agent, using an ideal rat model. Our long-term goal is to develop Cu-DOTA-alendronate for the detection and noninvasive differentiation of malignant versus benign breast tumors with PET. DOTA-alendronate was synthesized, radiolabeled with Cu, and administered to normal or tumor-bearing aged, female, retired breeder Sprague-Dawley rats for PET imaging. Mammary tissues were subsequently labeled and imaged with light, confocal, and electron microscopy to verify microcalcification targeting specificity of DOTA-alendronate and elucidate the histologic and ultrastructural characteristics of the microcalcifications in different mammary tumor types. Tumor uptake, biodistribution, and dosimetry studies were performed to evaluate the efficacy and safety of Cu-DOTA-alendronate. Cu-DOTA-alendronate was radiolabeled with a 98% yield. PET imaging using aged, female, retired breeder rats showed specific binding of Cu-DOTA-alendronate in mammary glands and mammary tumors. The highest uptake of Cu-DOTA-alendronate was in malignant tumors and the lowest uptake in benign tumors and normal mammary tissue. Confocal analysis with carboxyfluorescein-alendronate confirmed the microcalcification binding specificity of alendronate derivatives. Biodistribution studies revealed tissue alendronate concentrations peaking within the first hour, then decreasing over the next 48 h. Our dosimetric analysis demonstrated a Cu effective dose within the acceptable range for clinical PET imaging agents and the potential for translation into human patients. Cu-DOTA-alendronate is a promising PET imaging agent for the sensitive and specific detection of mammary tumors as well as the differentiation of malignant versus benign tumors based on absolute labeling uptake.
[Mh] Termos MeSH primário: Alendronato/química
Calcinose/diagnóstico por imagem
Radioisótopos de Cobre
Compostos Heterocíclicos com 1 Anel/química
Neoplasias Mamárias Experimentais/diagnóstico por imagem
Tomografia por Emissão de Pósitrons
[Mh] Termos MeSH secundário: Animais
Calcinose/metabolismo
Linhagem Celular Tumoral
Modelos Animais de Doenças
Feminino
Neoplasias Mamárias Experimentais/metabolismo
Ratos
Ratos Sprague-Dawley
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Copper Radioisotopes); 0 (Heterocyclic Compounds, 1-Ring); 1HTE449DGZ (1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid); X1J18R4W8P (Alendronate)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:180301
[Lr] Data última revisão:
180301
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE
[do] DOI:10.2967/jnumed.117.190850


  4 / 1529 MEDLINE  
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[PMID]:29177263
[Au] Autor:Cheki M; Gali H
[Ad] Endereço:Department of Radiologic Technology, Faculty of Paramedicine, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran. mohsencheky@gmail.com.
[Ti] Título:Primary radiation dosimetry of a novel PET radiopharmaceutical Ga-NODAGA-glycine in comparison with Tc-DTPA in renal studies.
[So] Source:Hell J Nucl Med;20(3):241-246, 2017 Sep-Dec.
[Is] ISSN:1790-5427
[Cp] País de publicação:Greece
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: In this study, we tried to estimate human absorbed dose of Ga-NODAGA-glycine as a new potential positron emission tomography (PET) renal agent based on the biodistribution data reported in healthy rats, and compare our estimation with the available absorbed dose data from technetium-99m-diethylenetriaminepentaacetic acid ( Tc-DTPA). SUBJECTS AND METHODS: The medical internal radiation dose (MIRD) formulation was applied to extrapolate from rats to human and to project the absorbed radiation dose for various organs in humans. S factor calculated by Monte-Carlo N-particle (MCNP) simulation and also this factor has been taken from the tables presented in MIRD pamphlet No.11. Hence, two radiation absorbed dose were calculated for organs. RESULTS: Our dose prediction shows that an 185MBq injection of gallium-68-1,4,7-triazacyclononane-1-γ-glutamylglycine-4,7-diacetic acid ( Ga-NODAGA-glycine) in humans might result in an estimated absorbed dose of 0.063mGy in the whole body when S factor calculated by MCNP simulation. The highest absorbed doses are observed in kidneys, lungs, spleen, liver, and red marrow with 3.510, 0.453, 0.335, 0.268, and 0.239mGy, respectively. In addition to, the estimated absorbed dose for total body after injection of 185MBq of Ga-NODAGA-glycine is 0.053mGy when S factor has been taken from MIRD pamphlet No.11. The highest absorbed doses are observed in kidneys, lungs, liver, spleen, and red marrow with 3.110, 0.438, 0.209, 0.203, and 0.203mGy, respectively. Comparison between human absorbed dose estimation for Ga-NODAGA-glycine and Tc-DTPA indicated that the absorbed dose of the most organs after injection of Tc-DTPA is higher than the amount after Ga-NODAGA-glycine. CONCLUSION: The results showed that Ga-NODAGA-glycine delivers lower dose to the patients. Also due to its application in PET (which offers higher sensitivity and spatial resolution compared to planar or SPET), Ga-NODAGA-glycine would be a superior choice than Tc-DTPA for renography and impose less radiation doses to patients.
[Mh] Termos MeSH primário: Absorção de Radiação/fisiologia
Complexos de Coordenação/farmacocinética
Glicina/análogos & derivados
Compostos Heterocíclicos com 1 Anel/farmacocinética
Rim/metabolismo
Modelos Biológicos
Tomografia por Emissão de Pósitrons/métodos
Radiometria/métodos
Pentetato de Tecnécio Tc 99m/farmacocinética
[Mh] Termos MeSH secundário: Animais
Simulação por Computador
Glicina/farmacocinética
Seres Humanos
Rim/diagnóstico por imagem
Especificidade de Órgãos/fisiologia
Projetos Piloto
Dose de Radiação
Exposição à Radiação/análise
Compostos Radiofarmacêuticos/farmacocinética
Ratos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (68Ga-NODAGA-glycine); 0 (Coordination Complexes); 0 (Heterocyclic Compounds, 1-Ring); 0 (Radiopharmaceuticals); TE7660XO1C (Glycine); VW78417PU1 (Technetium Tc 99m Pentetate)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE
[do] DOI:10.1967/s002449910609


  5 / 1529 MEDLINE  
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[PMID]:29181896
[Au] Autor:Yang X; Li S; Wang Z; Lee SMY; Wang LH; Wang R
[Ad] Endereço:State Key Laboratory of Quality Research in Chinese Medicine, and Institute of Chinese Medical Sciences, University of Macau, Avenida da Universidade, Taipa, Macau, China.
[Ti] Título:Constraining the Teratogenicity of Pesticide Pollution by a Synthetic Nanoreceptor.
[So] Source:Chem Asian J;13(1):41-45, 2018 Jan 04.
[Is] ISSN:1861-471X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:The teratogenicity of the pesticide nereistoxin (NTX) and its derivative thiocyclam (THI) towards aquatic life was dramatically constrained by a synthetic nanoreceptor, cucurbit[7]uril, through selective encapsulation of the pesticides (K of 3.24(±0.31)×10 m and K of 7.46(±0.10)×10 m ), as evidenced by the rate of hatchability, morphology development, and tyrosinase activity of zebrafish larvae incubated with the pesticides (3-300 µm) in the absence and in the presence of 300 µm cucurbit[7]uril, demonstrating the significant potential of the nanoreceptor in managing ecological pollution of these pesticides.
[Mh] Termos MeSH primário: Hidrocarbonetos Aromáticos com Pontes/farmacologia
Compostos Heterocíclicos com 1 Anel/antagonistas & inibidores
Compostos Heterocíclicos com 1 Anel/toxicidade
Imidazóis/farmacologia
Toxinas Marinhas/antagonistas & inibidores
Toxinas Marinhas/toxicidade
Teratogênios/toxicidade
Poluentes Químicos da Água/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Hidrocarbonetos Aromáticos com Pontes/química
Relação Dose-Resposta a Droga
Compostos Heterocíclicos com 1 Anel/química
Imidazóis/química
Larva/efeitos dos fármacos
Toxinas Marinhas/química
Estrutura Molecular
Relação Estrutura-Atividade
Teratogênios/química
Poluentes Químicos da Água/química
Poluentes Químicos da Água/toxicidade
Peixe-Zebra
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bridged-Ring Compounds); 0 (Heterocyclic Compounds, 1-Ring); 0 (Imidazoles); 0 (Marine Toxins); 0 (N,N-dimethyl-1,2,3-trithian-5-yl amine); 0 (Teratogens); 0 (Water Pollutants, Chemical); 0 (cucurbit(7)uril); 1631-58-9 (nereistoxin)
[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:171129
[St] Status:MEDLINE
[do] DOI:10.1002/asia.201701527


  6 / 1529 MEDLINE  
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[PMID]:28917649
[Au] Autor:Xu J; Feng C; Miao Y
[Ad] Endereço:Department of Radiology, School of Medicine, University of Colorado Denver, Aurora, CO 80045, USA.
[Ti] Título:Evaluation of novel In-labeled gonadotropin-releasing hormone peptides for human prostate cancer imaging.
[So] Source:Bioorg Med Chem Lett;27(20):4647-4651, 2017 10 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The purpose of this study was to evaluate the tumor targeting and imaging properties of novel In-labeled gonadotropin-releasing hormone (GnRH) peptides for human prostate cancer. Three new 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-linker-d-Phe-(d-Lys -GnRH) peptides with different hydrocarbon linkers were designed to evaluate their effects on GnRH receptor binding affinities. The Aoc (aminooctanoic acid) linker was better than ßAla (3-aminopropanoic acid) and Aun (aminoundecanoic acid) linkers in retaining strong receptor binding affinity. DOTA-Aoc-d-Phe-(d-Lys -GnRH) exhibited 6.6±0.1nM GnRH receptor binding affinity. In-DOTA-Aoc-d-Phe-(d-Lys -GnRH) exhibited fast tumor uptake and urinary clearance in DU145 human prostate cancer-xenografted nude mice. The DU145 tumor lesions could be clearly visualized by single photon emission computed tomography (SPECT)/CT using In-DOTA-Aoc-d-Phe-(d-Lys -GnRH) as an imaging probe, providing an insight into the design of new GnRH peptides for prostate cancer in the future.
[Mh] Termos MeSH primário: Hormônio Liberador de Gonadotropina/química
Neoplasias da Próstata/diagnóstico por imagem
Compostos Radiofarmacêuticos/química
Tomografia Computadorizada com Tomografia Computadorizada de Emissão de Fóton Único
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Animais
Linhagem Celular Tumoral
Cromatografia Líquida de Alta Pressão
Complexos de Coordenação/química
Hormônio Liberador de Gonadotropina/metabolismo
Compostos Heterocíclicos com 1 Anel/química
Seres Humanos
Radioisótopos de Índio/química
Masculino
Camundongos
Camundongos Nus
Ligação Proteica
Compostos Radiofarmacêuticos/metabolismo
Compostos Radiofarmacêuticos/urina
Distribuição Tecidual
Transplante Heterólogo
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Coordination Complexes); 0 (Heterocyclic Compounds, 1-Ring); 0 (Indium Radioisotopes); 0 (Radiopharmaceuticals); 0 (indium-111-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid); 33515-09-2 (Gonadotropin-Releasing Hormone)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170918
[St] Status:MEDLINE


  7 / 1529 MEDLINE  
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[PMID]:28750319
[Au] Autor:Min CG; Ferreira PJO; Pinto da Silva L
[Ad] Endereço:Research Center for Analysis and Measurement, Kunming University of Science and Technology, Kunming 650093, PR China.
[Ti] Título:Theoretically obtained insight into the mechanism and dioxetanone species responsible for the singlet chemiexcitation of Coelenterazine.
[So] Source:J Photochem Photobiol B;174:18-26, 2017 Sep.
[Is] ISSN:1873-2682
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Coelenterazine is a widespread bioluminescent substrate for a diverse set of marine species. Moreover, its imidazopyrazinone core is present in eight phyla of bioluminescent organisms. Given their very attractive intrinsic properties, these bioluminescent systems have been used in bioimaging, photodynamic therapy of cancer, as gene reporter and in sensing applications, among others. While it is known that bioluminescence results from the thermolysis of high-energy dioxetanones, the mechanism and dioxetanone species responsible for the singlet chemiexcitation of Coelenterazine are not fully understood. The theoretical characterization of the reactions of model Coelenterazine dioxetanones showed that efficient chemiexcitation is caused by a neutral dioxetanone with limited electron and charge transfer, by accessing a region of the PES where ground and excited states are nearly-degenerated. This finding was supported by calculation of equilibrium constants, which showed that only neutral dioxetanone is present in conditions associated with bioluminescence. Moreover, while cationic amino-acids easily protonate amide dioxetanone, anionic ones cannot deprotonate the neutral species. These results indicate that, contrary to existent theories, efficient chemiexcitation can occur with significant electron and/or charge transfer. In fact, these processes can be prejudicial to chemiexcitation, as anionic dioxetanones showed a less efficient chemiexcitation despite the occurrence of significant electron and charge transfer.
[Mh] Termos MeSH primário: Compostos Heterocíclicos com 1 Anel/química
Imidazóis/química
Modelos Químicos
Pirazinas/química
[Mh] Termos MeSH secundário: Amidas/química
Transporte de Elétrons
Luminescência
Modelos Moleculares
Conformação Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amides); 0 (Heterocyclic Compounds, 1-Ring); 0 (Imidazoles); 0 (Pyrazines); 0 (dioxetanone); 3O1CB88RRD (coelenterazine); 7GBN705NH1 (imidazole)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171012
[Lr] Data última revisão:
171012
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170728
[St] Status:MEDLINE


  8 / 1529 MEDLINE  
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[PMID]:28692297
[Au] Autor:Blank BR; Gut J; Rosenthal PJ; Renslo AR
[Ad] Endereço:Department of Pharmaceutical Chemistry and ‡Department of Medicine, University of California San Francisco , 1700 Fourth Street, San Francisco, California 94158, United States.
[Ti] Título:Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
[So] Source:J Med Chem;60(14):6400-6407, 2017 Jul 27.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We describe the first systematic study of antimalarial 1,2,4-trioxolanes bearing a substitution pattern regioisomeric to that of arterolane. Conformational analysis suggested that trans-3″-substituted trioxolanes would exhibit Fe(II) reactivity and antiparasitic activity similar to that achieved with canonical cis-4″ substitution. The chiral 3″ analogues were prepared as single stereoisomers and evaluated alongside their 4″ congeners against cultured malaria parasites and in a murine malaria model. As predicted, the trans-3″ analogues exhibited in vitro antiplasmodial activity remarkably similar to that of their cis-4″ comparators. In contrast, efficacy in the Plasmodium berghei mouse model differed dramatically for some of the congeneric pairs. The best of the novel 3″ analogues (e.g., 12i) outperformed arterolane itself, producing cures in mice after a single oral exposure. Overall, this study suggests new avenues for modulating Fe(II) reactivity and the pharmacokinetic and pharmacodynamic properties of 1,2,4-trioxolane antimalarials.
[Mh] Termos MeSH primário: Antimaláricos/química
Compostos Heterocíclicos com 1 Anel/química
Peróxidos/química
Compostos de Espiro/química
[Mh] Termos MeSH secundário: Animais
Antimaláricos/farmacologia
Antimaláricos/uso terapêutico
Feminino
Compostos Ferrosos/metabolismo
Compostos Heterocíclicos com 1 Anel/farmacologia
Compostos Heterocíclicos com 1 Anel/uso terapêutico
Malária/tratamento farmacológico
Malária/parasitologia
Camundongos
Peróxidos/farmacologia
Peróxidos/uso terapêutico
Plasmodium berghei
Plasmodium falciparum/efeitos dos fármacos
Plasmodium falciparum/metabolismo
Compostos de Espiro/farmacologia
Compostos de Espiro/uso terapêutico
Estereoisomerismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antimalarials); 0 (Ferrous Compounds); 0 (Heterocyclic Compounds, 1-Ring); 0 (Peroxides); 0 (Spiro Compounds); 3N1TN351VB (arterolane)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170906
[Lr] Data última revisão:
170906
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170711
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jmedchem.7b00699


  9 / 1529 MEDLINE  
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[PMID]:28655418
[Au] Autor:Chilla SNM; Zemek O; Kotek J; Boutry S; Larbanoix L; Sclavons C; Elst LV; Lukes I; Muller RN; Laurent S
[Ad] Endereço:Department of General, Organic and Biomedical Chemistry, NMR and Molecular Imaging Laboratory, University of Mons, Avenue Maistriau, 19, Mendeleïev Building, 7000 Mons, Belgium. Electronic address: satya.chilla@umons.ac.be.
[Ti] Título:Synthesis and characterization of monophosphinic acid DOTA derivative: A smart tool with functionalities for multimodal imaging.
[So] Source:Bioorg Med Chem;25(16):4297-4303, 2017 Aug 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A new facile synthetic strategy was developed to prepare bifunctional monophosphinic acid Ln-DOTA derivatives, Gd-DO2AGAP and Gd- DO2AGAP . The relaxivities of the Gd-complexes are enhanced compared to Gd-DOTA. Monophosphinic acid arm of these Gd-complexes affords enhancement of inner sphere water exchange rate due to its steric bulkiness. The different functionalities of DO2AGAP were appended in trans positions and are designed to conjugate identical or different vectors according to the potential applications. The conjugation of Gd-DO2AGAP with E3 peptide known to target apoptosis was successfully performed and in vivo MRI allowed cell death detection in a mouse model.
[Mh] Termos MeSH primário: Meios de Contraste/química
Compostos Heterocíclicos com 1 Anel/química
Imagem Multimodal
[Mh] Termos MeSH secundário: Animais
Meios de Contraste/síntese química
Relação Dose-Resposta a Droga
Feminino
Compostos Heterocíclicos com 1 Anel/síntese química
Imagem por Ressonância Magnética
Camundongos
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Contrast Media); 0 (Heterocyclic Compounds, 1-Ring); 1HTE449DGZ (1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170814
[Lr] Data última revisão:
170814
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170629
[St] Status:MEDLINE


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[PMID]:28628723
[Au] Autor:Vultos F; Fernandes C; Mendes F; Marques F; Correia JDG; Santos I; Gano L
[Ad] Endereço:Centro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, km 139.7, 2695-066, Bobadela, LRS, Portugal.
[Ti] Título:A Multifunctional Radiotheranostic Agent for Dual Targeting of Breast Cancer Cells.
[So] Source:ChemMedChem;12(14):1103-1107, 2017 Jul 20.
[Is] ISSN:1860-7187
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:A straightforward synthetic route for a new multifunctional 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) derivative is described. To demonstrate the versatility of this pro-chelator for the preparation of radiolabeled hybrid compounds containing two different biological targeting moieties, an antitumor agent (e.g., a DNA-intercalating agent) and an estrogen receptor (ER) ligand (e.g., LXXLL-based peptide) were regiospecifically conjugated to the DOTA derivative. The bifunctional probe was radiolabeled with the auger electron emitter indium-111, and the resulting radioconjugate was demonstrated to induce DNA damage in vitro, which, along with the nuclear internalization exhibited in breast cancer cells, might enhance its therapeutic activity. This favorable in vitro performance suggests that these hybrid compounds could be attractive probes for theranostic applications.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Compostos Aza/síntese química
Compostos Heterocíclicos com 1 Anel/síntese química
Compostos Radiofarmacêuticos/síntese química
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/farmacologia
Compostos Aza/farmacologia
Neoplasias da Mama
Sobrevivência Celular/efeitos dos fármacos
Quelantes/química
Feminino
Compostos Heterocíclicos com 1 Anel/farmacologia
Seres Humanos
Radioisótopos de Índio
Substâncias Intercalantes/química
Ligantes
Células MCF-7
Camundongos
Peptídeos/química
Ligação Proteica
Compostos Radiofarmacêuticos/farmacologia
Receptores Estrogênicos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetracetic acid); 0 (Antineoplastic Agents); 0 (Aza Compounds); 0 (Chelating Agents); 0 (Heterocyclic Compounds, 1-Ring); 0 (Indium Radioisotopes); 0 (Intercalating Agents); 0 (Ligands); 0 (Peptides); 0 (Radiopharmaceuticals); 0 (Receptors, Estrogen)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170620
[St] Status:MEDLINE
[do] DOI:10.1002/cmdc.201700287



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