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Id: lil-794674
Autor: Coelho, Rafael Corrêa; Reinert, Tomás; Campos, Franz; Peixoto, Fábio Affonso; Andrade, Carlos Augusto de; Castro, Thalita; Herchenhorn, Daniel.
Título: Sunitinib treatment in patients with advanced renal cell cancer: the Brazilian National Cancer Institute (INCA) experience
Fonte: Int. braz. j. urol;42(4):694-703, July-Aug. 2016. tab, graf.
Idioma: en.
Resumo: ABSTRACT Purpose: The aim of this study was to assess the impact of sunitinib treatment in a non-screened group of patients with metastatic renal cell cancer (mRCC) treated by the Brazilian Unified Health System (SUS) at a single reference institution. Material and Methods: Retrospective cohort study, which evaluated patients with mRCC who received sunitinib between May 2010 and December 2013. Results: Fifty-eight patients were eligible. Most patients were male 41 (71%), with a median age of 58 years. Nephrectomy was performed in 41 (71%) patients with a median interval of 16 months between the surgery and initiation of sunitinib. The most prevalent histological subtype was clear cell carcinoma, present in 52 (91.2%) patients. In 50 patients (86%), sunitinib was the first line of systemic treatment. The main adverse effects were fatigue (57%), hypothyroidism (43%), mucositis (33%) and diarrhea (29%). Grade 3 and 4 adverse effects were infrequent: fatigue (12%), hypertension (12%), thrombocytopenia (7%), neutropenia (5%) and hand-foot syndrome (5%). Forty percent of patients achieved a partial response and 35% stable disease, with a disease control rate of 75%. Median progression free survival was 7.6 months and median overall survival was 14.1 months. Conclusion: Sunitinib treatment was active in the majority of patients, especially those with low and intermediate risk by MSKCC score, with manageable toxicity. Survival rates were inferior in this non-screened population with mRCC treated in the SUS.
Descritores: Pirróis/uso terapêutico
Carcinoma de Células Renais/tratamento farmacológico
Indóis/uso terapêutico
Neoplasias Renais/tratamento farmacológico
Antineoplásicos/uso terapêutico
-Pirróis/efeitos adversos
Brasil
Carcinoma de Células Renais/secundário
Estudos Retrospectivos
Intervalo Livre de Doença
Sunitinibe
Programas Governamentais
Indóis/efeitos adversos
Neoplasias Renais/patologia
Neoplasias Pulmonares/secundário
Metástase Linfática
Pessoa de Meia-Idade
Programas Nacionais de Saúde
Antineoplásicos/efeitos adversos
Limites: Humanos
Masculino
Feminino
Adolescente
Adulto
Idoso
Idoso de 80 Anos ou mais
Adulto Jovem
Responsável: BR1.1 - BIREME


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Id: biblio-1129749
Autor: Acosta, A. C; Santos, A. S; Silva, F. A. G; Medeiros, E. S; Oliveira, H. P. de; Costa, M. M; Fernandes, A. W. C; Pinheiro Júnior, J. W; Mota, R. A.
Título: Atividade antibacteriana de nanopartículas de polipirrol diante de Staphylococcus aureus isolados de amostras de leite de vacas e cabras com mastite / Antibacterial behavior of polypyrrole nanoparticles against Staphylococcus aureus isolated from cows and goats with mastitis
Fonte: Arq. bras. med. vet. zootec. (Online);72(3):1047-1050, May-June, 2020. ilus.
Idioma: pt.
Projeto: Fundação de Amparo à Ciência e Tecnologia de Pernambuco; . Conselho Nacional de Desenvolvimento Científico e Tecnológico.
Resumo: The aim of the present study was to evaluate the antibacterial behavior of polypyrrole nanoparticles (PPy-NPs) in water against biofilm producer or not S. aureus isolated from cows and goats with mastitis. One hundred and thirty-eight isolates of S. aureus were initially evaluated for biofilm formation by spectrophotometry in microplates. In addition, the minimum inhibition concentration (MIC) and minimum bactericidal concentration (MBC) of PPy-NPs in water for planktonic S. aureus were determined. From the bovine samples analyzed, 5 (4.46%) S. aureus isolates showed a strong biofilm production, 17 (15.18%) moderate production, 36 (32.14%) with weak production and 54 (48.21%) did not produce biofilms. Strains from goats (26) showed no biofilm production in 18 (69.23%) strains and weak biofilm production in 8 (30.76%) strains. The MIC and MBC of S. aureus to PPy-NPs were found in the same concentration (125搭/mL) in all strains tested, regardless of biofilm production or not. This finding provides a new insight into the interaction between PPy-NPs and S. aureus, and will offer potential benefits for the control of mastitis.(AU)
Descritores: Pirróis/administração & dosagem
Staphylococcus aureus/efeitos dos fármacos
Cabras/microbiologia
Mastite/veterinária
-Biofilmes
Antibacterianos/uso terapêutico
Limites: Animais
Feminino
Bovinos
Responsável: BR68.1 - Biblioteca Virginie Buff D'Ápice


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Id: biblio-838413
Autor: Canu, Letizia; Pradella, Silvia; Rapizzi, Elena; Fucci, Rossella; Valeri, Andrea; Briganti, Vittorio; Giachè, Valentino; Parenti, Gabriele; Ercolino, Tonino; Mannelli, Massimo.
Título: Sunitinib in the therapy of malignant paragangliomas: report on the efficacy in a SDHB mutation carrier and review of the literature
Fonte: Arch. endocrinol. metab. (Online);61(1):90-97, Jan.-Feb. 2017. tab, graf.
Idioma: en.
Resumo: SUMMARY Metastatic pheochromocytomas (PHEOs) and paragangliomas (sPGLs) are rare neural crest-derived tumors with a poor prognosis. About 50% of them are due to germ-line mutations of the SDHB gene. At present, there is no cure for these tumors. Their therapy is palliative and represented by different options among which antiangiogenic drugs, like sunitinib, have been hypothesized to be effective especially in malignant SDHB mutated tumors. We report the effects of sunitinib therapy in a SDHB mutation carrier affected by a malignant sPGL. During 101 weeks of therapy at different doses, sunitinib was able to cause a partial response and then a stable disease for a total of 78 weeks. This favorable response is the longest, out of the 35 so far reported in the literature, registered in a patient treated exclusively with sunitinib but, similarly to the other responses, the effect was limited in time. From our analysis of the scanty data present in the literature, the effect of sunitinib does not seem to be different among wild-type patients and those carrying a cluster 1 germ-line mutation. Sunitinib seems able to slow the disease progression in some patients with malignant PHEO/PGL and therefore may represent a therapeutic option, although randomized controlled studies are needed to assess its efficacy definitively in the treatment of these aggressive tumors.
Descritores: Paraganglioma/tratamento farmacológico
Pirróis/uso terapêutico
Inibidores da Angiogênese/uso terapêutico
Indóis/uso terapêutico
Mutação/genética
Antineoplásicos/uso terapêutico
-Paraganglioma/genética
Paraganglioma/irrigação sanguínea
Succinato Desidrogenase/genética
Resultado do Tratamento
Sunitinibe
Metástase Neoplásica
Limites: Humanos
Masculino
Adulto
Tipo de Publ: Relatos de Casos
Revisão
Responsável: BR1.1 - BIREME


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Id: biblio-887589
Autor: Valdes-Socin, Hernan; Almanza, Matilde Rubio; Fernández-Ladreda, Mariana Tomé; Daele, Daniel Van; Polus, Marc; Chavez, Marcela; Beckers, Albert.
Título: Use of cinacalcet and sunitinib to treat hypercalcaemia due to a pancreatic neuroendocrine tumor
Fonte: Arch. endocrinol. metab. (Online);61(5):506-509, Sept.-Oct. 2017. graf.
Idioma: en.
Resumo: SUMMARY Neuroendocrine tumors (NETs) can secrete hormones, including ectopic secretions, but they have been rarely associated with malignant hypercalcemia. A 52-year-old man with a history of diabetes mellitus was diagnosed with a pancreatic tumor. A pancreatic biopsy confirmed a well-differentiated pancreatic NET (pNET). The patient subsequently developed liver metastasis and hypercalcemia with high 1,25 OH vitamin D and suppressed parathyroid hormone (PTH) levels. Hypercalcemia was refractory to chemotherapy, intravenous saline fluids, diuretics, calcitonin and zoledronate. Cinacalcet administration (120 mg/day) resulted in a significant calcium reduction. Hypocalcemia was observed when sunitinib was added three months later and cinacalcet was stopped. Subsequently, the calcium and PTH levels normalized. After six months, we observed 20% shrinkage of the pancreatic tumor and necrosis of a liver metastasis. Cinacalcet is an allosteric activator of the calcium receptor agonist, and it is used for severe hypercalcemia in patients with primary (benign and malignant) hyperparathyroidism. In this patient, cinacalcet demonstrated a calcium lowering effect, normalized hypophosphatemia, and improved the clinical condition of the patient. The mechanism through which cinacalcet improved PTH-rp mediated hypercalcemia is still unclear, but studies have suggested that a potential mechanism is the activation of calcitonin secretion. Sunitinib is an oral multi-targeted tyrosine kinase inhibitor used to treat advanced pNETs. The hypocalcemic effects of sunitinib have not been previously described in a patient with pNET. Here, we report for the first time the successful combination of cinacalcet and sunitinib in the treatment of a pNET patient presenting with malignant hypercalcemia.
Descritores: Neoplasias Pancreáticas/tratamento farmacológico
Tumores Neuroendócrinos/tratamento farmacológico
Cinacalcete/administração & dosagem
Hipercalcemia/tratamento farmacológico
Indóis/administração & dosagem
Antineoplásicos/administração & dosagem
-Neoplasias Pancreáticas/complicações
Pirróis/administração & dosagem
Tumores Neuroendócrinos/complicações
Quimioterapia Combinada
Sunitinibe
Hipercalcemia/etiologia
Limites: Humanos
Masculino
Pessoa de Meia-Idade
Tipo de Publ: Relatos de Casos
Responsável: BR1.1 - BIREME


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Id: lil-596564
Autor: Aguilar, Cristian; Ventura, Freddy; Rodríguez-Delfín, Luis.
Título: El aumento de la expresión del ARNm de la enzima convertidora de angiotensina I homóloga (ECA-2) inducido por atorvastatina se asocia a menor fibrosis e hipertrofia ventricular izquierda en un modelo de cardiomiopatía diabética / Atorvastatin induced increase in homologous angiotensin i converting enzyme (ACE2) mRNA is associated to decreased fibrosis and decreased left ventricular hypertrophy in a rat model of diabetic cardiomyopathy
Fonte: Rev. peru. med. exp. salud publica;28(2):264-272, jun. 2011. ilus, graf, mapas, tab.
Idioma: es.
Resumo: Objetivos. Evaluar el efecto de atorvastatina sobre la progresión del remodelado cardiaco y la expresión de ECA-2 en el miocardio de ratas diabéticas. Materiales y métodos. La diabetes fue inducida en ratas Holtzman con una inyección intraperitoneal de estreptozotocina. Los animales fueron divididos en tres grupos: (1) ratas control, (2) ratas diabéticas y (3) ratas diabéticas tratadas con atorvastatina (50 mg/kg/día). Después de ocho semanas de tratamiento, los corazones fueron extraídos para el análisis morfométrico, la cuantificación de colágeno y la determinación de los niveles de ARNm de ECA y ECA-2. Resultados. El índice de hipertrofia ventricular y el depósito de colágeno se incrementaron significativamente en las ratas diabéticas. La administración de atorvastatina previno estos cambios sin modificar los niveles de colesterol. La hiperglicemia produjo un incremento significativo en los niveles del ARNm de ECA y una marcada disminución en la expresión de ECA-2 en el miocardio de ratas diabéticas. La administración de atorvastatina indujo la expresión del ARNm de ECA-2 e inhibió la sobreexpresión del ARNm de ECA en el miocardio de las ratas diabéticas. Conclusiones. Nuestros resultados indican que la atorvastatina, independientemente de su capacidad para disminuir el colesterol, normaliza la relación de la expresión de ECA/ECA-2 y atenúa el desarrollo del remodelado adverso en el corazón diabético.

Objectives. This study has investigated the effect of atorvastatin on the progression of cardiac remodelling and ACE- 2 expression in diabetic myocardium in rats. Materials and Methods. Diabetes was induced in Holtzman rats with an intraperitoneal injection of streptozotocin. The animals were divided into 3 groups: (1) normal control rats, (2) diabetic rats and (3) diabetic rats treated orally with atorvastatin (50 mg/kg/day). After eight weeks of treatment, the hearts were removed for morphometric studies, collagen content assay and genetic expressions of ACE and ACE2 mRNA. Results. Myocardial hypertrophy index and collagen deposition were increased in diabetic rats, but not in the treated-diabetic rats, without producing changes in cholesterol levels. Myocardial ACE mRNA levels were increased while ACE2 mRNA levels were decreased in diabetic rats. Atorvastatin administration attenuated overexpression of ACE mRNA and overexpression of ACE-2 mRNA in diabetic rats. Conclusions. Our results indicate that atorvastatin, independently of its cholesterol-lowering capacity, lowers the ACE/ACE2 ratio to normal values and attenuates the development of adverse remodeling in the diabetic heart.
Descritores: Cardiomiopatias Diabéticas/genética
Cardiomiopatias Diabéticas/prevenção & controle
Ácidos Heptanoicos/uso terapêutico
Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico
Hipertrofia Ventricular Esquerda/genética
Peptidil Dipeptidase A/genética
Pirróis/uso terapêutico
RNA Mensageiro/biossíntese
RNA Mensageiro/efeitos dos fármacos
-Modelos Animais de Doenças
Fibrose/genética
Fibrose/prevenção & controle
Ratos Sprague-Dawley
Limites: Animais
Masculino
Ratos
Responsável: BR1.1 - BIREME


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Id: lil-418874
Autor: Borges, Jairo Lins.
Título: Combinação de fármacos na abordagem das dislipidemias: associação entre estatinas e niacina / Combination of drugs: statins and niacin
Fonte: Arq. bras. cardiol;85(supl.5):36-41, out. 2005. tab, graf.
Idioma: pt.
Resumo: A combinação de estatinas com niacina se apresenta como uma atraente associação, na presença de dislipidemia mista com níveis de HDL baixo, quando monoterapia é insuficiente para o alcance das metas lipídicas. Benefícios clínicos foram observados com a combinação de estatinas com niacina nos estudos FATS, HATS e ARBITER 2, mostrando atenuação no desenvolvimento da aterosclerose e/ou redução de eventos coronários, acompanhados de alterações lipídicas favoráveis. Em geral, esta combinação é bem tolerada. Recomenda-se monitoração adequada das enzimas hepáticas e muscular e, ainda, titulação cuidadosa de cada uma das drogas combinadas.
Descritores: Dislipidemias/tratamento farmacológico
Inibidores de Hidroximetilglutaril-CoA Redutases/efeitos adversos
Inibidores de Hidroximetilglutaril-CoA Redutases/metabolismo
Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico
Niacina/uso terapêutico
-Aterosclerose/tratamento farmacológico
Aterosclerose/metabolismo
HDL-Colesterol/sangue
LDL-Colesterol/sangue
Dislipidemias/metabolismo
Distribuição por Idade
Fatores Sexuais
Interações Medicamentosas
Niacina/efeitos adversos
Niacina/metabolismo
Pirróis/efeitos adversos
Pirróis/metabolismo
Pirróis/uso terapêutico
Quimioterapia Combinada
Sinvastatina/efeitos adversos
Sinvastatina/metabolismo
Sinvastatina/uso terapêutico
Ácidos Heptanoicos/efeitos adversos
Ácidos Heptanoicos/metabolismo
Ácidos Heptanoicos/uso terapêutico
Responsável: BR1.1 - BIREME


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Id: lil-408367
Autor: Rodrigues, A. C; Rebecchi, I. M. M; Bertolami, M. C; Faludi, A. A; Hirata, M. H; Hirata, R. D. C.
Título: High baseline serum total and LDL cholesterol levels are associated with MDR1 haplotypes in Brazilian hypercholesterolemic individuals of European descent
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;38(9):1389-1397, Sept. 2005. tab, graf.
Idioma: en.
Projeto: Fundação de Amparo à Pesquisa do Estado de São Paulo; . Conselho Nacional de Desenvolvimento Científico e Tecnológico.
Resumo: The MDR1 gene encodes the P-glycoprotein, an efflux transporter with broad substrate specificity. P-glycoprotein has raised great interest in pharmacogenetics because it transports a variety of structurally divergent drugs, including lipid-lowering drugs. The synonymous single-nucleotide polymorphism C3435T and the nonsynonymous single-nucleotide polymorphism G2677T/A in MDR1 have been indicated as potential determinants of variability in drug disposition and efficacy. In order to evaluate the effect of G2677T/A and C3435T MDR1 polymorphisms on serum levels of lipids before and after atorvastatin administration, 69 unrelated hypercholesterolemic individuals from São Paulo city, Brazil, were selected and treated with 10 mg atorvastatin orally once daily for four weeks. MDR1 polymorphisms were analyzed by PCR-RFLP. C3435T and G2677T polymorphisms were found to be linked. The allelic frequencies for C3435T polymorphism were 0.536 and 0.464 for the 3435C and 3435T alleles, respectively, while for G2677T/A polymorphism allele frequencies were 0.580 for the 2677G allele, 0.384 for the 2677T allele and 0.036 for the 2677A allele. There was no significant relation between atorvastatin response and MDR1 polymorphisms (repeated measures ANOVA; P > 0.05). However, haplotype analysis revealed an association between T/T carriers and higher basal serum total (TC) and LDL cholesterol levels (TC: 303 ± 56, LDL-C: 216 ± 57 mg/dl, respectively) compared with non-T/T carriers (TC: 278 ± 28, LDL-C: 189 ± 24 mg/dl; repeated measures ANOVA/Tukey test; P < 0.05). These data indicate that MDR1 polymorphism may have an important contribution to the control of basal serum cholesterol levels in Brazilian hypercholesterolemic individuals of European descent.
Descritores: LDL-Colesterol/sangue
Genes MDR/genética
Haplótipos/genética
Hipercolesterolemia/genética
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/genética
-Anticolesterolemiantes/uso terapêutico
Brasil
LDL-Colesterol/genética
Grupo com Ancestrais do Continente Europeu
Frequência do Gene
Ácidos Heptanoicos/uso terapêutico
Hipercolesterolemia/sangue
Hipercolesterolemia/tratamento farmacológico
Hipercolesterolemia/etnologia
Reação em Cadeia da Polimerase
Polimorfismo Genético
Polimorfismo de Fragmento de Restrição
Polimorfismo de Nucleotídeo Único
Pirróis/uso terapêutico
Limites: Adulto
Idoso
Feminino
Humanos
Masculino
Pessoa de Meia-Idade
Responsável: BR1.1 - BIREME


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Laurindo, Iêda Maria Magalhäes
Xavier, Ricardo Machado
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Id: lil-770015
Autor: Mota, Licia Maria Henrique da; Cruz, Bóris Afonso; Albuquerque, Cleandro Pires de; Gonçalves, Deborah Pereira; Laurindo, Ieda Maria Magalhães; Pereira, Ivanio Alves; Carvalho, Jozélio Freire de; Pinheiro, Geraldo da Rocha Castelar; Bertolo, Manoel Barros; Pinto, Maria Raquel da Costa; Louzada-Junior, Paulo; Xavier, Ricardo Machado; Giorgi, Rina Dalva Neubarth; Lima, Rodrigo Aires Corrêa.
Título: Posicionamento sobre o uso de tofacitinibe no algoritmo do Consenso 2012 da Sociedade Brasileira de Reumatologia para o tratamento da artrite reumatoide / Update on the 2012 Brazilian Society of Rheumatology Guidelines for the treatment of rheumatoid arthritis: position on the use of tofacitinib
Fonte: Rev. bras. reumatol;55(6):512-521, nov.-dez. 2015. graf.
Idioma: en.
Resumo: Resumo Em 2014, o tofacitinibe, um medicamento modificador do curso da doença (MMCD) sintético, alvo-específico, inibidor seletivo das Janus quinases (JAK), foi aprovado para uso no Brasil. Este documento de posicionamento tem o objetivo de atualizar as recomendações da Sociedade Brasileira de Reumatologia (SBR) sobre o tratamento da artrite reumatoide (AR) no Brasil, especificamente com relação ao uso de MMCD sintéticos alvo-específicos. O método dessa recomendação incluiu revisão bibliográfica de artigos científicos, feita na base de dados Medline. Após a revisão, foi produzido um texto, que responde a perguntas na estrutura Pico, e considera questões de eficácia e segurança do uso do tofacitinibe para tratamento de AR em diferentes situações (como primeira linha de tratamento, após falha ao metotrexato [MTX] ou outros MMCD sintéticos convencionais, após falha da terapia biológica). Com base nas evidências existentes, e considerando os dados disponíveis sobre eficácia, segurança e custo das medicações disponíveis para tratamento da doença no Brasil, a Comissão de AR da SBR, após processo de discussão e votação de propostas, estabeleceu o seguinte posicionamento sobre o uso de tofacitinibe para o tratamento da AR no Brasil: “Tofacitinibe, em monoterapia ou em associação ao MTX, é uma opção para os pacientes com AR em atividade moderada ou alta, após falha de pelo menos dois esquemas com diferentes MMCD sintéticos e um esquema de MMCD biológico”. O grau de concordância com essa recomendação foi 7,5. Esse posicionamento poderá ser revisto nos próximos anos, com a maior experiência adquirida com o uso do medicamento.

Abstract In 2014, tofacitinib, a target-specific, synthetic disease modifying anti rheumatic drug (DMARD) and a selective inhibitor of Janus kinase (JAK) was approved for use in Brazil. This position paper aims to update the recommendations of the Brazilian Society of Rheumatology (SBR) on the treatment of rheumatoid arthritis (RA) in Brazil, specifically regarding the use of target-specific synthetic DMARDs. The method of this recommendation consisted of a literature review of scientific papers held on the Medline database. After this review, a text was produced, answering questions in Pico structure, considering efficacy and safety issues of tofacitinib use for RA treatment in different scenarios (such as first-line treatment after failure with methotrexate [MTX] or other conventional synthetic DMARDs after failure with biological therapy). Based on existing evidence, and considering the available data on efficacy, safety and cost of medications available to treat the disease in Brazil, the RA Commission of SBR, after a process of discussion and voting on proposals, established the following position on the use of tofacitinib for treatment of RA in Brazil: “Tofacitinib, alone or in combination with MTX, is an alternative for RA patients with moderate or high activity after failure of at least two different synthetic DMARDs and one biological DMARD.” The level of agreement with this recommendation was 7.5. This position may be reviewed in the coming years, in the face of a greater experience with the use of this medication.
Descritores: Piperidinas/uso terapêutico
Artrite Reumatoide/tratamento farmacológico
Pirimidinas/uso terapêutico
Pirróis/uso terapêutico
Antirreumáticos/uso terapêutico
-Reumatologia
Sociedades Médicas
Brasil
Metotrexato/uso terapêutico
Falha de Tratamento
Quimioterapia Combinada
Limites: Humanos
Responsável: BR1.1 - BIREME


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Id: biblio-1001583
Autor: El-Sharkawy, Karam Ahmed; AlBratty, Mohammed Mofreh; Alhazmi, Hassan Ahmad.
Título: Synthesis of some novel pyrimidine, thiophene, coumarin, pyridine and pyrrole derivatives and their biological evaluation as analgesic, antipyretic and anti-inflammatory agents
Fonte: Braz. J. Pharm. Sci. (Online);54(4):e00153, 2018. tab, graf.
Idioma: en.
Resumo: Pyrimidine derivative 3 was afforded through the reaction of compound (1) with 5-ureidohydantion (2). Product 3 underwent a cyclization to produce fused pyrimidine derivative 7, although the latter product 7 was synthesized through one step via the reaction of compound (1) with 5-ureidohydantion (2) using another catalyst. Compound 3 was oriented to react with cyclic ketones 8a,b in the presence of elemental sulfur, salicylaldehyde (10), aryldiazonium chlorides 12a,b and ω-bromo-4-methoxy- acetophenone (14), which afforded, fused thiophene derivatives 9a,b, coumarin derivative 11, arylhdrazono derivatives 13a,b and 4-methoxyphenyl butenyl derivative 15, respectively. The latter product 15 was reacted with either potassium cyanide (16a) or potassium thiocyanide (16b) to form cyano and thiocyano derivatives 17a,b, respectively. Compound 17a underwent further cyclization to afford pyridopyrimidine derivative 19. Compound 15 was reacted with either hydrazine (20a) or phenylhydrazine (20b) to produce hydrazo derivatives 21a,b and these products were cyclize to produce pyrrole derivatives 23a,b. Finally, 5-ureidohydantion (2) was reacted with compounds 24a,b,c to afford pyrimidine derivatives 25a,b,c. The structures of the synthesized compounds were confirmed using IR, 1H NMR, 13C NMR and mass spectrometry techniques. Compounds 11 and 19 have promising as analgesic and antipyretic activities
Descritores: Piridinas/análise
Pirimidinas/agonistas
Pirróis
Tiofenos/análise
Cumarínicos/análise
-Antipiréticos
Analgésicos/classificação
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: biblio-955116
Autor: Rogerio, Kamilla Rodrigues; Carvalho, Leonardo J M; Domingues, Luiza Helena Pinto; Neves, Bruno Junior; Moreira Filho, José Teófilo; Castro, Rosane Nora; Bianco Júnior, Cesare; Daniel-Ribeiro, Claudio Tadeu; Andrade, Carolina Horta; Graebin, Cedric Stephan.
Título: Synthesis and molecular modelling studies of pyrimidinones and pyrrolo[34-d]-pyrimidinodiones as new antiplasmodial compounds
Fonte: Mem. Inst. Oswaldo Cruz;113(8):e170452, 2018. tab, graf.
Idioma: en.
Resumo: BACKGROUND Malaria is responsible for 429,000 deaths per year worldwide, and more than 200 million cases were reported in 2015. Increasing parasite resistance has imposed restrictions to the currently available antimalarial drugs. Thus, the search for new, effective and safe antimalarial drugs is crucial. Heterocyclic compounds, such as dihydropyrimidinones (DHPM), synthesised via the Biginelli multicomponent reaction, as well as bicyclic compounds synthesised from DHPMs, have emerged as potential antimalarial candidates in the last few years. METHODS Thirty compounds were synthesised employing the Biginelli multicomponent reaction and subsequent one-pot substitution/cyclisation protocol; the compounds were then evaluated in vitro against chloroquine-resistant Plasmodium falciparum parasites (W2 strain). Drug cytotoxicity in baseline kidney African Green Monkey cells (BGM) was also evaluated. The most active in vitro compounds were evaluated against P. berghei parasites in mice. Additionally, we performed an in silico target fishing approach with the most active compounds, aiming to shed some light into the mechanism at a molecular level. RESULTS The synthetic route chosen was effective, leading to products with high purity and yields ranging from 10-84%. Three out of the 30 compounds tested were identified as active against the parasite and presented low toxicity. The in silico study suggested that among all the molecular targets identified by our target fishing approach, Protein Kinase 3 (PK5) and Glycogen Synthase Kinase 3β (GSK-3β) are the most likely molecular targets for the synthesised compounds. CONCLUSIONS We were able to easily obtain a collection of heterocyclic compounds with in vitro anti-P. falciparum activity that can be used as scaffolds for the design and development of new antiplasmodial drugs.
Descritores: Desenho de Fármacos
Testes de Sensibilidade Parasitária
Antimaláricos/síntese química
Antimaláricos/farmacologia
-Pirimidinonas
Pirróis
Responsável: BR1.1 - BIREME



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