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[PMID]:28888123
[Au] Autor:Tot A; Vranes M; Maksimovic I; Putnik-Delic M; Danicic M; Belic S; Gadzuric S
[Ad] Endereço:University of Novi Sad, Faculty of Sciences, Department of Chemistry, Biochemistry and Environmental Protection, Trg D. Obradovica 3, 21000 Novi Sad, Serbia.
[Ti] Título:The effect of imidazolium based ionic liquids on wheat and barley germination and growth: Influence of length and oxygen functionalization of alkyl side chain.
[So] Source:Ecotoxicol Environ Saf;147:401-406, 2018 Jan.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:In this work five different imidazolium based ionic liquids, namely: 1-(2-oxybutyl)-3-methylimidazolium chloride, [C OC mIm][Cl]; 1-(2-oxypropyl)-3-methylimidazolium chloride, [C OC mIm][Cl]; 1-(3-hydroxypropyl)-3-ethylimidazolium chloride, [OHC eIm][Cl]; 1-(3-hydroxypropyl)-3-methylimidazolium chloride, [OHC mIm][Cl]; 1-(2-hydroxyethyl)-3-methylimidazolium chloride, [OHC mIm][Cl], together with commercial 1-butyl-3-methylimidazolium chloride, [bmim][Cl] and synthesized protic imidazolium chloride, [Im][Cl], were prepared and their toxicity examined towards wheat and barley germination and growth. Introduction of the polar groups (in the form of hydroxyde and/or ether group) in the alkyl side chain of the imidazolium cation and their influence on the reduction of the ionic liquid's toxicity is demonstrated. The results indicate that toxicity of oxygen functionalized ILs is significantly lower against wheat comparing to non-functionalized analogues. In the case of barley, influence on germination follow the same trend as in the case of wheat, but for seedlings growth different trend is observed with more pronounced toxicity of ether functionalized ILs. From these results it was also shown that alkylation in the position N-3 atom of the imidazole significantly reduces toxicity of cation.
[Mh] Termos MeSH primário: Germinação/efeitos dos fármacos
Hordeum/efeitos dos fármacos
Imidazóis/toxicidade
Líquidos Iônicos/toxicidade
Oxigênio/química
Triticum/efeitos dos fármacos
[Mh] Termos MeSH secundário: Cátions
Hordeum/crescimento & desenvolvimento
Imidazóis/síntese química
Imidazóis/química
Líquidos Iônicos/síntese química
Líquidos Iônicos/química
Estrutura Molecular
Plântulas/efeitos dos fármacos
Plântulas/crescimento & desenvolvimento
Triticum/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cations); 0 (Imidazoles); 0 (Ionic Liquids); 41PS77334A (1-butyl-3-methylimidazolium chloride); 7GBN705NH1 (imidazole); S88TT14065 (Oxygen)
[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:170910
[St] Status:MEDLINE


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[PMID]:29403337
[Au] Autor:Umunakwe OC; Herren D; Kim SJ; Kohanim S
[Ad] Endereço:Department of Ophthalmology and Visual Sciences, Vanderbilt University Medical Center, Nashville, Tennessee.
[Ti] Título:Diffuse ocular and orbital inflammation after zoledronate infusion-case report and review of the literature.
[So] Source:Digit J Ophthalmol;23(4):18-21, 2017.
[Is] ISSN:1542-8958
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Bisphosphonates have become a commonly used class of medications to treat osteoporosis and other bone diseases. Zoledronate (zoledronic acid) can be dosed annually via intravenous infusion, making it an appealing option for patients and physicians. We report the case of a 68-year-old woman who developed severe, unilateral, ocular inflammation, including corneal endotheliitis, anterior uveitis with hyphema, scleritis, and orbital inflammation beginning 12 hours after receiving her first zoledronate infusion. Symptoms escalated but ultimately resolved with topical steroids and high-dose systemic corticosteroids. To our knowledge, this is the first report of unilateral diffuse inflammation of the eye and orbit, including corneal inflammation developing within 12 hours of a first zoledronate infusion.
[Mh] Termos MeSH primário: Difosfonatos/efeitos adversos
Imidazóis/efeitos adversos
Doenças Orbitárias/induzido quimicamente
Osteoporose/tratamento farmacológico
Uveíte Anterior/induzido quimicamente
[Mh] Termos MeSH secundário: Doença Aguda
Idoso
Conservadores da Densidade Óssea/administração & dosagem
Conservadores da Densidade Óssea/efeitos adversos
Difosfonatos/administração & dosagem
Feminino
Seres Humanos
Imidazóis/administração & dosagem
Inflamação/induzido quimicamente
Inflamação/diagnóstico
Infusões Intravenosas
Doenças Orbitárias/diagnóstico
Tomografia Computadorizada por Raios X
Uveíte Anterior/diagnóstico
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Bone Density Conservation Agents); 0 (Diphosphonates); 0 (Imidazoles); 6XC1PAD3KF (zoledronic acid)
[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:180207
[St] Status:MEDLINE
[do] DOI:10.5693/djo.02.2017.08.002


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[PMID]:29412148
[Au] Autor:Hou J; Cui C; Kim S; Sung C; Choi C
[Ad] Endereço:Intelligent Synthetic Biology Center, Daejeon 34141, Republic of Korea.
[Ti] Título:Ginsenoside F1 suppresses astrocytic senescence-associated secretory phenotype.
[So] Source:Chem Biol Interact;283:75-83, 2018 Mar 01.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Senescence is one of the hallmarks of aging and identified as a potential therapeutic target in the treatment of aging and aging-related diseases. Senescent cells accumulate with age in a variety of human tissues where they develop a complex senescence-associated secretory phenotype (SASP). SASP in brain could contribute to age-related inflammation and chronic neurodegenerative diseases. We confirmed that senescent astrocytes express a characteristic of SASP in vitro by human cytokine antibody array. Ginsenoside F1 suppresses the SASP from astrocytes induced by d-galactose via suppressing p38MAPK-dependent NF-κB activity. A specific inhibitor of p38MAPK, SB203580 significantly decreased the secretion of IL-6 and IL-8, the major components of SASPs. Additionally, treatment of senescent astrocytes with NF-κB inhibitor, BAY 11-7092, also suppressed the secretion of IL-6 and IL-8, suggesting NF-κB was required for SASP. Importantly, conditioned media from senescent astrocytes promoted the migration of glioblastoma cells, such as U373-MG, U251-MG and U87-MG assessed by scratch wound healing. This migration was significantly decreased by F1 treatment in senescent astrocytes. Interestingly, IL-8, the main mediator regulating glioblastoma cell invasion, was suppressed in both transcriptional and protein level. Herein, we propose ginsenoside F1 as a potential therapeutic strategy for reducing the deleterious contribution of senescent astrocytes in aged brain and related diseases.
[Mh] Termos MeSH primário: Senescência Celular/efeitos dos fármacos
Ginsenosídeos/farmacologia
[Mh] Termos MeSH secundário: Astrócitos/citologia
Astrócitos/efeitos dos fármacos
Astrócitos/metabolismo
Linhagem Celular
Movimento Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Reparo do DNA/efeitos dos fármacos
Ensaio de Imunoadsorção Enzimática
Seres Humanos
Imidazóis/farmacologia
Interleucina-6/análise
Interleucina-6/metabolismo
Interleucina-8/análise
Interleucina-8/metabolismo
NF-kappa B/antagonistas & inibidores
NF-kappa B/metabolismo
Fosforilação/efeitos dos fármacos
Piridinas/farmacologia
Transdução de Sinais/efeitos dos fármacos
Proteínas Quinases p38 Ativadas por Mitógeno/antagonistas & inibidores
Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ginsenosides); 0 (Imidazoles); 0 (Interleukin-6); 0 (Interleukin-8); 0 (NF-kappa B); 0 (Pyridines); 53963-43-2 (ginsenoside F1); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); OU13V1EYWQ (SB 203580)
[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:180208
[St] Status:MEDLINE


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[PMID]:29331859
[Au] Autor:Albiol-Chiva J; Esteve-Romero J; Peris-Vicente J
[Ad] Endereço:Departament de Química Física i Analítica, Universitat Jaume I, 12071 Castelló, Spain.
[Ti] Título:Development of a method to determine axitinib, lapatinib and afatinib in plasma by micellar liquid chromatography and validation by the European Medicines Agency guidelines.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1074-1075:61-69, 2018 Feb 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A method based on micellar liquid chromatography to quantify the tyrosine kinase inhibitors axitinib, lapatinib and afatinib in plasma is reported. The sample pretreatment was a simple 1/5-dilution in a pure micellar solution, filtration and direct injection, without requiring extraction or purification steps. The three drugs were resolved from the matrix in 17min, using an aqueous solution of 0.07M sodium dodecyl sulfate - 6.0% 1-pentanol, buffered at pH7 with 0.01M phosphate salt as mobile phase, running under isocratic mode at 1mL/min through a C18 column. The detection was performed by absorbance at 260nm. An accurate mathematical relationship was established between the retention factor of each drug and the surfactant/organic solvent concentration in the mobile phase, achieved with a limited number of experiments, in order to optimize these factors. A binding behavior of the analytes face to the micelles was found out. The method was successfully validated by the guidelines of the European Medicines Agency in terms of: selectivity, linearity (r >0.9995), calibration range (0.5 to 10mg/L), limit of detection (0.2mg/L), carry-over effect, accuracy (-8.1 to +6.9%), precision (<13.8%), dilution integrity, matrix effect, stability and robustness. The procedure was found reliable, practical, economic, accessible, short-time, easy-to-handle, inexpensive, environmental-friendly, safe, useful for the analysis of many samples per day. Finally, the method was applied to the analysis of incurred, using quality control samples in the same analytical run, with adequate results. Therefore, it can be implementable for routine analysis in clinical laboratories.
[Mh] Termos MeSH primário: Cromatografia Líquida/métodos
Imidazóis/sangue
Indazóis/sangue
Quinazolinas/sangue
[Mh] Termos MeSH secundário: Antineoplásicos/sangue
Antineoplásicos/uso terapêutico
Estabilidade de Medicamentos
Seres Humanos
Imidazóis/uso terapêutico
Indazóis/uso terapêutico
Limite de Detecção
Modelos Lineares
Micelas
Neoplasias/tratamento farmacológico
Quinazolinas/uso terapêutico
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Imidazoles); 0 (Indazoles); 0 (Micelles); 0 (Quinazolines); 0VUA21238F (lapatinib); 41UD74L59M (afatinib); C9LVQ0YUXG (axitinib)
[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:180115
[St] Status:MEDLINE


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[PMID]:28464864
[Au] Autor:Shimazu K; Tada Y; Morinaga T; Shingyoji M; Sekine I; Shimada H; Hiroshima K; Namiki T; Tatsumi K; Tagawa M
[Ad] Endereço:Department of Respirology, Graduate School of Medicine, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba, 260-8670, Japan.
[Ti] Título:Metformin produces growth inhibitory effects in combination with nutlin-3a on malignant mesothelioma through a cross-talk between mTOR and p53 pathways.
[So] Source:BMC Cancer;17(1):309, 2017 May 02.
[Is] ISSN:1471-2407
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Mesothelioma is resistant to conventional treatments and is often defective in p53 pathways. We then examined anti-tumor effects of metformin, an agent for type 2 diabetes, and combinatory effects of metformin and nutlin-3a, an inhibitor for ubiquitin-mediated p53 degradation, on human mesothelioma. METHODS: We examined the effects with a colorimetric assay and cell cycle analyses, and investigated molecular events in cells treated with metformin and/or nutlin-3a with Western blot analyses. An involvement of p53 was tested with siRNA for p53. RESULTS: Metformin suppressed cell growth of 9 kinds of mesothelioma including immortalized cells of mesothelium origin irrespective of the p53 functional status, whereas susceptibility to nutlin-3a was partly dependent on the p53 genotype. We investigated combinatory effects of metformin and nutlin-3a on, nutlin-3a sensitive MSTO-211H and NCI-H28 cells and insensitive EHMES-10 cells, all of which had the wild-type p53 gene. Knockdown of p53 expression with the siRNA demonstrated that susceptibility of MSTO-211H and NCI-H28 cells to nutlin-3a was p53-dependent, whereas that of EHMES-10 cells was not. Nevertheless, all the cells treated with both agents produced additive or synergistic growth inhibitory effects. Cell cycle analyses also showed that the combination increased sub-G1 fractions greater than metformin or nutlin-3a alone in MSTO-211H and EHMES-10 cells. Western blot analyses showed that metformin inhibited downstream pathways of the mammalian target of rapamycin (mTOR) but did not activate the p53 pathways, whereas nutlin-3a phosphorylated p53 and suppressed mTOR pathways. Cleaved caspase-3 and conversion of LC3A/B were also detected but it was dependent on cells and treatments. The combination of both agents in MSTO-211H cells rather suppressed the p53 pathways that were activated by nutrin-3a treatments, whereas the combination rather augmented the p53 actions in NCI-H28 and EHMES-10 cells. CONCLUSION: These data collectively indicated a possible interactions between mTOR and p53 pathways, and the combinatory effects were attributable to differential mechanisms induced by a cross-talk between the pathways.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Imidazóis/farmacologia
Neoplasias Pulmonares/metabolismo
Mesotelioma/metabolismo
Metformina/farmacologia
Piperazinas/farmacologia
Serina-Treonina Quinases TOR/metabolismo
Proteína Supressora de Tumor p53/metabolismo
[Mh] Termos MeSH secundário: Ciclo Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Seres Humanos
Transdução de Sinais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Imidazoles); 0 (Piperazines); 0 (Tumor Suppressor Protein p53); 53IA0V845C (nutlin 3); 9100L32L2N (Metformin); EC 2.7.1.1 (MTOR protein, human); EC 2.7.1.1 (TOR Serine-Threonine Kinases)
[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:170504
[St] Status:MEDLINE
[do] DOI:10.1186/s12885-017-3300-y


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[PMID]:27775691
[Au] Autor:Hendrix MJ; Kandela I; Mazar AP; Seftor EA; Seftor RE; Margaryan NV; Strizzi L; Murphy GF; Long GV; Scolyer RA
[Ad] Endereço:Department of Biology, Shepherd University, Shepherdstown, WV, USA.
[Ti] Título:Targeting melanoma with front-line therapy does not abrogate Nodal-expressing tumor cells.
[So] Source:Lab Invest;97(2):176-186, 2017 02.
[Is] ISSN:1530-0307
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Metastatic melanoma is a highly aggressive skin cancer with a poor prognosis. It is the leading cause of skin cancer deaths with a median overall survival for advanced-stage metastatic disease of <6 months. Despite advances in the field with conventional and targeted therapies, the heterogeneity of melanoma poses the greatest ongoing challenge, ultimately leading to relapse and progression to a more drug-resistant tumor in most patients. Particularly noteworthy are recent findings, indicating that these therapies exert selective pressure on tumors resulting in the activation of pathways associated with cancer stem cells that are unresponsive to current therapy. Our previous studies have shown how Nodal, an embryonic morphogen of the transforming growth factor-beta superfamily, is one of these critical factors that is reactivated in aggressive melanoma and resistant to conventional chemotherapy, such as dacarbazine. In the current study, we sought to determine whether BRAF inhibitor (BRAFi) therapy targeted Nodal-expressing tumor cells in uniquely matched unresectable stage III and IV melanoma patient samples before and after therapy that preceded their eventual death due to disease. The results demonstrate that BRAFi treatment failed to affect Nodal levels in melanoma tissues. Accompanying experiments in soft agar and in nude mice showed the advantage of using combinatorial treatment with BRAFi plus anti-Nodal monoclonal antibody to suppress tumor growth and metastasis. These data provide a promising new approach using front-line therapy combined with targeting a cancer stem cell-associated molecule-producing a more efficacious response than monotherapy.
[Mh] Termos MeSH primário: Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico
Melanoma/tratamento farmacológico
Proteína Nodal/antagonistas & inibidores
Proteínas Proto-Oncogênicas B-raf/antagonistas & inibidores
Neoplasias Cutâneas/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Anticorpos Monoclonais/administração & dosagem
Western Blotting
Linhagem Celular Tumoral
Feminino
Seres Humanos
Imidazóis/administração & dosagem
Imuno-Histoquímica
Neoplasias Pulmonares/prevenção & controle
Neoplasias Pulmonares/secundário
Melanoma/genética
Melanoma/metabolismo
Camundongos Nus
Terapia de Alvo Molecular/métodos
Mutação
Proteína Nodal/imunologia
Proteína Nodal/metabolismo
Oximas/administração & dosagem
Proteínas Proto-Oncogênicas B-raf/genética
Proteínas Proto-Oncogênicas B-raf/metabolismo
Piridonas/administração & dosagem
Pirimidinonas/administração & dosagem
Neoplasias Cutâneas/genética
Neoplasias Cutâneas/metabolismo
Resultado do Tratamento
Ensaios Antitumorais Modelo de Xenoenxerto/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Antibodies, Monoclonal); 0 (Imidazoles); 0 (Nodal Protein); 0 (Oximes); 0 (Pyridones); 0 (Pyrimidinones); 33E86K87QN (trametinib); EC 2.7.11.1 (Proto-Oncogene Proteins B-raf); QGP4HA4G1B (dabrafenib)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:180306
[Lr] Data última revisão:
180306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161025
[St] Status:MEDLINE
[do] DOI:10.1038/labinvest.2016.107


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[PMID]:29329002
[Au] Autor:Durdagi S; Aksoydan B; Erol I; Kantarcioglu I; Ergun Y; Bulut G; Acar M; Avsar T; Liapakis G; Karageorgos V; Salmas RE; Sergi B; Alkhatib S; Turan G; Yigit BN; Cantasir K; Kurt B; Kilic T
[Ad] Endereço:Computational Biology and Molecular Simulations Laboratory, Department of Biophysics, School of Medicine, Bahcesehir University (BAU), Istanbul, Turkey; Neuroscience Program, Graduate School of Health Sciences, Bahcesehir University, Istanbul, Turkey. Electronic address: serdar.durdagi@med.bau.edu.t
[Ti] Título:Integration of multi-scale molecular modeling approaches with experiments for the in silico guided design and discovery of novel hERG-Neutral antihypertensive oxazalone and imidazolone derivatives and analysis of their potential restrictive effects on cell proliferation.
[So] Source:Eur J Med Chem;145:273-290, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:AT1 antagonists is the most recent drug class of molecules against hypertension and they mediate their actions through blocking detrimental effects of angiotensin II (A-II) when acts on type I (AT1) A-II receptor. The effects of AT1 antagonists are not limited to cardiovascular diseases. AT1 receptor blockers may be used as potential anti-cancer agents - due to the inhibition of cell proliferation stimulated by A-II. Therefore, AT1 receptors and the A-II biosynthesis mechanisms are targets for the development of new synthetic drugs and therapeutic treatment of various cardiovascular and other diseases. In this work, multi-scale molecular modeling approaches were performed and it is found that oxazolone and imidazolone derivatives reveal similar/better interaction energy profiles compared to the FDA approved sartan molecules at the binding site of the AT1 receptor. In silico-guided designed hit molecules were then synthesized and tested for their binding affinities to human AT1 receptor in radioligand binding studies, using [ I-Sar -Ile ] AngII. Among the compounds tested, 19d and 9j molecules bound to receptor in a dose response manner and with relatively high affinities. Next, cytotoxicity and wound healing assays were performed for these hit molecules. Since hit molecule 19d led to deceleration of cell motility in all three cell lines (NIH3T3, A549, and H358) tested in this study, this molecule is investigated in further tests. In two cell lines (HUVEC and MCF-7) tested, 19d induced G2/M cell cycle arrest in a concentration dependent manner. Adherent cells detached from the plates and underwent cell death possibly due to apoptosis at 19d concentrations that induced cell cycle arrest.
[Mh] Termos MeSH primário: Anti-Hipertensivos/farmacologia
Antineoplásicos/farmacologia
Descoberta de Drogas
Canais de Potássio Éter-A-Go-Go/antagonistas & inibidores
Imidazóis/farmacologia
Oxazolona/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Hipertensivos/síntese química
Anti-Hipertensivos/química
Antineoplásicos/síntese química
Antineoplásicos/química
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Morte Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Células Cultivadas
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Canais de Potássio Éter-A-Go-Go/metabolismo
Seres Humanos
Imidazóis/síntese química
Imidazóis/química
Camundongos
Modelos Moleculares
Estrutura Molecular
Células NIH 3T3
Oxazolona/síntese química
Oxazolona/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antihypertensive Agents); 0 (Antineoplastic Agents); 0 (Ether-A-Go-Go Potassium Channels); 0 (Imidazoles); 0 (KCNH1 protein, human); 0 (imidazolone); 15646-46-5 (Oxazolone)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180113
[St] Status:MEDLINE


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[PMID]:29291439
[Au] Autor:Vanda D; Soural M; Canale V; Chaumont-Dubel S; Satala G; Kos T; Funk P; Fülöpová V; Lemrová B; Koczurkiewicz P; Pekala E; Bojarski AJ; Popik P; Marin P; Zajdel P
[Ad] Endereço:Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, 5 Hnevotínská Street, 779-00 Olomouc, Czech Republic.
[Ti] Título:Novel non-sulfonamide 5-HT receptor partial inverse agonist in a group of imidazo[4,5-b]pyridines with cognition enhancing properties.
[So] Source:Eur J Med Chem;144:716-729, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A small library of novel 3H-imidazo[4,5-b]pyridine and 1H-imidazo[4,5-c]pyridine derivatives was designed and synthesized as non-sulfonamide 5-HT receptor ligands. In vitro evaluation allowed to identify compound 17 (2-ethyl-3-(3-fluorobenzyl)-7-(piperazin-1-yl)-3H-imidazo[4,5-b]pyridine) as potent 5-HT receptor partial inverse agonist in G signaling (K = 6 nM, IC = 17.6 nM). Compound 17 displayed high metabolic stability, favorable cytochrome P450 isoenzyme (2D6, 3A4) profile, did not affect PgP-protein binding, without evoking mutagenic effects. It was orally bioavailable and brain penetrant. In contrast to intepirdine (SB-742457), which prevented 5-HT R-elicited neurite growth and behaved as an inverse agonist of cyclin-dependent kinase 5 (Cdk5), compound 17 has no influence on neuronal differentiation. Compound 17 exerted significant pro-cognitive properties in novel object recognition (NOR) task in rats reversing both phencyclidine- and scopolamine-induced memory deficits (MED = 1 and 0.3 mg/kg, p.o, respectively). These effects were similar to those produced by intepirdine. Additionally, combination of inactive doses of compound 17 (0.1 mg/kg) and donepezil (0.3 mg/kg) produced synergistic effect to reverse scopolamine-induced memory deficits. Accordingly, investigating putative divergence between inverse agonists and neutral antagonists as cognitive enhancers in neurodegenerative and psychiatric disorders is certainly of utmost interest.
[Mh] Termos MeSH primário: Cognição/efeitos dos fármacos
Imidazóis/farmacologia
Piridinas/farmacologia
Receptores de Serotonina/metabolismo
[Mh] Termos MeSH secundário: Animais
Relação Dose-Resposta a Droga
Células HEK293
Seres Humanos
Imidazóis/síntese química
Imidazóis/química
Masculino
Estrutura Molecular
Piridinas/síntese química
Piridinas/química
Ratos
Ratos Sprague-Dawley
Ratos Wistar
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Imidazoles); 0 (Pyridines); 0 (Receptors, Serotonin); 0 (imidazo(4,5-b)pyridine); 0 (serotonin 6 receptor)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180102
[St] Status:MEDLINE


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[PMID]:29276983
[Au] Autor:Notari S; Tempestilli M; Fabbri G; Libertone R; Antinori A; Ammassari A; Agrati C
[Ad] Endereço:Laboratory of Cellular Immunology and Pharmacology, National Institute for Infectious Diseases "Lazzaro Spallanzani", IRCCS, Rome, Italy.
[Ti] Título:UPLC-MS/MS method for the simultaneous quantification of sofosbuvir, sofosbuvir metabolite (GS-331007) and daclatasvir in plasma of HIV/HCV co-infected patients.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1073:183-190, 2018 Jan 15.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Direct-acting antiviral agents (DAAs) represent the major advance in hepatitis C virus (HCV) infection treatment leading to extremely high eradication rates in HCV mono- and HIV/HCV co-infected patients. In this scenery, availability of Therapeutic Drug Monitoring (TDM) is of interest to assess plasma concentrations to prevent either therapeutic failure due to suboptimal medication adherence and drug-drug interactions or avoid adverse events. Aim of this study was to develop and validate an Ultra-Performance Liquid Chromatography Mass Spectrometry (UPLC-MS/MS) method for the simultaneous quantification of sofosbuvir, sofosbuvir metabolite (GS-331007), and daclatasvir in human plasma. A simple protein precipitation was applied by adding 200 µL acetonitrile with internal standard 6,7-Dimethyl- 2,3-di(2-pyridyl) quinoxaline to 100 µL plasma sample. Drug separation was performed on analytical C-18 Luna Omega column (50 mm × 2.1 mm I.D.) with particle size of 1.6 µm. The mobile phase consisting of water containing 0.1% formic acid and acetonitrile at flow 0.4 mL/min and a gradient run time of 3.5 min. The injection volume was 10 µL. Anti-HCV drugs were detected in positive electrospray ionization mode. The full scan mass spectral analyses of sofosbuvir, GS-331007, daclatasvir and quinaxoline showed protonated molecule ions and transitions m/z: 530.098 → 243.02, 260.93 → 112.94, 739.4 → 339.27 and 313.03 → 77.99 respectively. The linearity of standard curves was excellent (r > 0.99), the absolute recovery of anti-HCV drugs ranged between 95 and 98%, and both imprecision and inaccuracy were <15% according to FDA guidelines. The UPLC-MS/MS method was applied to 16 plasma samples of as many HIV/HCV co-infected patients treated with sofosbuvir and daclatasvir. While sofosbuvir was not detectable in all samples, the median plasma concentrations of daclatasvir and GS-331007 were 223.6 ±â€¯319.56 ng/mL and 537.11 ±â€¯242.09 ng/mL, respectively. In conclusion, we describe an UPLC-MS/MS method allowing the simultaneous quantification of sofosbuvir, GS-331007 and daclatasvir in plasma samples. The method was sensitive, specific, robust, and time-saving.
[Mh] Termos MeSH primário: Antivirais/sangue
Coinfecção/tratamento farmacológico
Infecções por HIV/tratamento farmacológico
Hepatite C/tratamento farmacológico
Imidazóis/sangue
Sofosbuvir/sangue
[Mh] Termos MeSH secundário: Cromatografia Líquida de Alta Pressão/métodos
Seres Humanos
Limite de Detecção
Modelos Lineares
Reprodutibilidade dos Testes
Sofosbuvir/análogos & derivados
Sofosbuvir/química
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (BMS-790052); 0 (Imidazoles); WJ6CA3ZU8B (Sofosbuvir)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171226
[St] Status:MEDLINE


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[PMID]:29191265
[Au] Autor:Gobbato AAM; Gobbato CARS; Moreno RA; Antunes NJ; De Nucci G
[Ti] Título:Dapaconazole versus ketoconazole in the treatment of interdigital tinea pedis.
[So] Source:Int J Clin Pharmacol Ther;56(1):31-33, 2018 Jan.
[Is] ISSN:0946-1965
[Cp] País de publicação:Germany
[La] Idioma:eng
[Mh] Termos MeSH primário: Antifúngicos/uso terapêutico
Imidazóis/uso terapêutico
Cetoconazol/uso terapêutico
Tinha dos Pés/tratamento farmacológico
[Mh] Termos MeSH secundário: Adulto
Feminino
Seres Humanos
Masculino
Meia-Idade
Pomadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1-(2-(2,4-dichlorophenyl)-2-(4-(trifluoromethyl)benzyloxy)ethyl)-1H-imidazole); 0 (Antifungal Agents); 0 (Imidazoles); 0 (Ointments); R9400W927I (Ketoconazole)
[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:171202
[St] Status:MEDLINE
[do] DOI:10.5414/CP203124



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