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[PMID]:23489645
[Au] Autor:Dore MP; Massidda M; Yilmaz O; Demiray-Gürbüz E; Manca A; Bassotti G
[Ad] Endereço:Dipartimento di Medicina Clinica e Sperimentale, University of Sassari, Sassari, Italy. mpdore@uniss.it
[Ti] Título:Miocamycin-containing triple therapy for H. pylori infection.
[So] Source:Helicobacter;18(4):285-9, 2013 Aug.
[Is] ISSN:1523-5378
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: In Northern Sardinia, one-week triple standard therapies containing a proton-pump inhibitor and two antibiotics for H. pylori infection have an average cure rate of 57% largely due to a high prevalence of antimicrobial resistance. The efficacy of miocamycin-containing treatment for 10 days was evaluated. MATERIALS AND METHODS: Patients referred to the endoscopy service for dyspeptic symptoms were enrolled. H. pylori infection was defined as a positive rapid urease test, presence of the bacteria on gastric biopsies, and a positive 13C-UBT. Treatment consisted of 10 days with omeprazole 20 mg, miocamycin water-soluble 900 mg, and tinidazole 500 mg all bid. Success was evaluated 40-50 days after the end of therapy and defined by a negative 13C-UBT. Compliance was considered good if at least 90% of the total number of the pills were taken. Fluorescent in situ hybridization (FISH) technique was applied on paraffin-embedded gastric tissue sections to test susceptibility to clarithromycin of the bacteria. RESULTS: 50 patients were enrolled (mean age; 52, 36% men). Miocamycin-containing therapy cured 86% (42/49; 95% CI = 72-94%) of infected patients by PP analysis. Susceptibility data (FISH) was available for 38 patients. Cure rates for the 28 with clarithromycin-susceptible infection was 96% vs 50% for those with resistant or mixed infection, (p = .003). Good compliance was recorded in 48 patients. None of the patients discontinued therapy. CONCLUSIONS: Miocamycin appears to be a valid alternative for clarithromycin for H. pylori eradication. Head-to-head studies will be needed to ascertain whether it is superior.
[Mh] Termos MeSH primário: Antibacterianos/administração & dosagem
Infecções por Helicobacter/tratamento farmacológico
Miocamicina/administração & dosagem
[Mh] Termos MeSH secundário: Adulto
Idoso
Testes Respiratórios
Quimioterapia Combinada/métodos
Feminino
Mucosa Gástrica/microbiologia
Helicobacter pylori/efeitos dos fármacos
Seres Humanos
Hibridização in Situ Fluorescente
Itália
Masculino
Testes de Sensibilidade Microbiana/métodos
Meia-Idade
Projetos Piloto
Resultado do Tratamento
Ureia/análise
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 3T48CPS7U2 (Miocamycin); 8W8T17847W (Urea)
[Em] Mês de entrada:1310
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:130316
[St] Status:MEDLINE
[do] DOI:10.1111/hel.12048


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[PMID]:24081472
[Au] Autor:Gavini E; Rassu G; Ferraro L; Generosi A; Rau JV; Brunetti A; Giunchedi P; Dalpiaz A
[Ad] Endereço:Department of Drug Sciences, University of Sassari, Sassari 07100, Italy.
[Ti] Título:Influence of chitosan glutamate on the in vivo intranasal absorption of rokitamycin from microspheres.
[So] Source:J Pharm Sci;100(4):1488-502, 2011 Apr.
[Is] ISSN:1520-6017
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Intranasal delivery is an alternative method to target therapeutics to the central nervous system. In the present study, chitosan glutamate (CG)-based mucoadhesive microspheres containing rokitamycin (RK) were prepared by spray-drying and in vitro characterization. Moreover, the influence of CG on RK absorption in bloodstream and cerebrospinal fluid (CSF) was evaluated after nasal administration to rats. The in vivo results were compared with those obtained after nasal administration of chitosan (CH)-based microparticles containing RK and after intravenous (IV) administration of the free drug. The in vitro results indicate that the concentrations of feed solution or kind of CH influence the RK entrapment and size of microspheres. All formulations increase the solubility of this poorly water-soluble drug, but CG is more able to increase the in vitro dissolution rate of RK than CH. CG microspheres absorb water quickly and then dissolve, whereas CH particles need more volume of water for swelling and gelling. In vivo studies showed that, after IV administration, RK is not able to cross the blood-brain barrier and to reach the CSF from the bloodstream. On the contrary, drug goes to the CSF and the bloodstream only after nasal administration of CG microparticles.
[Mh] Termos MeSH primário: Antibacterianos/administração & dosagem
Quitosana/química
Preparações de Ação Retardada/química
Ácido Glutâmico/química
Miocamicina/análogos & derivados
Absorção Nasal
[Mh] Termos MeSH secundário: Administração Intranasal
Animais
Antibacterianos/farmacocinética
Seres Humanos
Masculino
Microesferas
Miocamicina/administração & dosagem
Miocamicina/farmacocinética
Ratos
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Delayed-Action Preparations); 3KX376GY7L (Glutamic Acid); 3T48CPS7U2 (Miocamycin); 9012-76-4 (Chitosan); ZPT03UEM0E (rokitamycin)
[Em] Mês de entrada:1412
[Cu] Atualização por classe:131001
[Lr] Data última revisão:
131001
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:131002
[St] Status:MEDLINE
[do] DOI:10.1002/jps.22382


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[PMID]:21409489
[Au] Autor:Hiraki M; Kitajima Y; Koga Y; Tanaka T; Nakamura J; Hashiguchi K; Noshiro H; Miyazaki K
[Ad] Endereço:Department of Surgery, Saga University Faculty of Medicine, Saga, Japan.
[Ti] Título:Aberrant gene methylation is a biomarker for the detection of cancer cells in peritoneal wash samples from advanced gastric cancer patients.
[So] Source:Ann Surg Oncol;18(10):3013-9, 2011 Oct.
[Is] ISSN:1534-4681
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To assess whether gene methylation in peritoneal fluid (PF) is clinically feasible for determining micrometastasis to the peritoneum in gastric cancer. METHODS: The gene methylation of BNIP3, CHFR, CYP1B1, MINT25, SFRP2, and RASSF2 were analyzed in 107 specimens of PF by quantitative methylation-specific polymerase chain reaction. All patients were placed into one of 3 groups: group A (n = 42), patients with depth of cancer invasion at muscularis propria (MP) or less than MP; group B (n = 45), depth of cancer invasion beyond the MP; and group C (n = 20), histologically diagnosed peritoneal metastasis or cancer cells cytologically defined in the peritoneal cavity. Patients in both groups A and B were diagnosed as having no cancer cells by peritoneal cytology and histology. RESULTS: The methylation status of the 6 genes was found to be significantly different among the 3 groups (group A, 0-5%; group B, 0-15%; group C, 15-45%; P < 0.01). Furthermore, the rate of positive methylation in any of the 6 genes was significantly different in each group (group A, 7%; group B, 20%; group C, 75%; P < 0.001). Three of 9 patients in group B with positive methylation in any of 6 genes experienced peritoneal recurrence. On the other hand, only 1 of 36 patients without gene methylation experienced peritoneal recurrence (P < 0.05). CONCLUSIONS: DNA methylation in PFs is a possible marker detecting occult neoplastic cells on the peritoneum. Methylation analysis along with a cytological examination might therefore improve the positive detection of cancer cells in PF of gastric cancer.
[Mh] Termos MeSH primário: Biomarcadores Tumorais/genética
Metilação de DNA
Recidiva Local de Neoplasia/genética
Lavagem Peritoneal
Neoplasias Peritoneais/genética
Neoplasias Gástricas/genética
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Hidrocarboneto de Aril Hidroxilases/genética
Proteínas de Ciclo Celular/genética
Citocromo P-450 CYP1B1
DNA de Neoplasias/genética
Estudos de Viabilidade
Feminino
Mucosa Gástrica/metabolismo
Mucosa Gástrica/patologia
Seres Humanos
Masculino
Proteínas de Membrana/genética
Meia-Idade
Miocamicina
Micrometástase de Neoplasia
Proteínas de Neoplasias/genética
Recidiva Local de Neoplasia/diagnóstico
Estadiamento de Neoplasias
Neoplasias Peritoneais/secundário
Proteínas de Ligação a Poli-ADP-Ribose
Reação em Cadeia da Polimerase
Prognóstico
Proteínas Proto-Oncogênicas/genética
Neoplasias Gástricas/patologia
Taxa de Sobrevida
Células Tumorais Cultivadas
Proteínas Supressoras de Tumor/genética
Ubiquitina-Proteína Ligases
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (BNIP3 protein, human); 0 (Biomarkers, Tumor); 0 (Cell Cycle Proteins); 0 (DNA, Neoplasm); 0 (Membrane Proteins); 0 (Neoplasm Proteins); 0 (Poly-ADP-Ribose Binding Proteins); 0 (Proto-Oncogene Proteins); 0 (RASSF2 protein, human); 0 (SFRP2 protein, human); 0 (Tumor Suppressor Proteins); 3T48CPS7U2 (Miocamycin); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (CYP1B1 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP1B1); EC 2.3.2.27 (CHFR protein, human); EC 2.3.2.27 (Ubiquitin-Protein Ligases)
[Em] Mês de entrada:1201
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110317
[St] Status:MEDLINE
[do] DOI:10.1245/s10434-011-1636-0


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[PMID]:19747296
[Au] Autor:Mervic L; Dragos V; Pavlovic MD
[Ti] Título:Linear IgA bullous dermatosis of childhood: successful treatment with miocamycin and topical corticosteroid.
[So] Source:Clin Exp Dermatol;34(7):e391-2, 2009 Oct.
[Is] ISSN:1365-2230
[Cp] País de publicação:England
[La] Idioma:eng
[Mh] Termos MeSH primário: Doenças Autoimunes/diagnóstico
Glucocorticoides/uso terapêutico
Imunoglobulina A/análise
Miocamicina/uso terapêutico
Dermatopatias Vesiculobolhosas/diagnóstico
[Mh] Termos MeSH secundário: Antibacterianos/uso terapêutico
Betametasona/análogos & derivados
Betametasona/uso terapêutico
Quimioterapia Combinada
Seres Humanos
Lactente
Masculino
[Pt] Tipo de publicação:CASE REPORTS; LETTER
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Glucocorticoids); 0 (Immunoglobulin A); 3T48CPS7U2 (Miocamycin); 826Y60901U (betamethasone-17,21-dipropionate); 9842X06Q6M (Betamethasone)
[Em] Mês de entrada:1003
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090915
[St] Status:MEDLINE
[do] DOI:10.1111/j.1365-2230.2009.03366.x


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[PMID]:19479981
[Au] Autor:Rassu G; Gavini E; Jonassen H; Zambito Y; Fogli S; Breschi MC; Giunchedi P
[Ad] Endereço:Department of Drug Sciences, University of Sassari, via Muroni 23/A, 07100 Sassari, Italy.
[Ti] Título:New chitosan derivatives for the preparation of rokitamycin loaded microspheres designed for ocular or nasal administration.
[So] Source:J Pharm Sci;98(12):4852-65, 2009 Dec.
[Is] ISSN:1520-6017
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Acanthamoeba spp. are the causative agents of granulomatous amoebic encephalitis (GAE) and amoebic keratitis. Recent studies performed by Rassu et al. showed that, compared with the free drug, the loading of rokitamycin in chitosan microspheres improves and prolongs the in vitro antiamoebic activity of rokitamycin. This could be useful in transporting the drug for either ocular application to treat amoebic keratitis or nasal administration as an alternative route for the administration of the drug to the brain in GAE therapy. Starting from the previous study, our goal was to optimize the technological parameters in order to obtain chitosan microparticles loaded with rokitamycin and to evaluate the use of new quaternary ammonium chitosan derivatives in the preparation of spray dried microspheres containing the macrolide; these derivatives showed better characteristics (solubility, penetration enhancement) compared with chitosan itself. Toxicity studies on new polymers were performed. Spray dried loaded microspheres based on chitosan or chitosan derivatives were obtained by using appropriate preparative parameters. Microparticles containing chitosan derivatives showed similar or often better properties than formulations made of chitosan with respect to size, in vitro release behaviour and mucoadhesiveness thus making them more suitable for ocular or nasal administration. New polymers did not demonstrate cytotoxicity.
[Mh] Termos MeSH primário: Antiprotozoários/administração & dosagem
Antiprotozoários/química
Quitosana/química
Miocamicina/análogos & derivados
[Mh] Termos MeSH secundário: Adesividade
Administração Intranasal
Adesão Celular
Sobrevivência Celular/efeitos dos fármacos
Composição de Medicamentos
Células Endoteliais/efeitos dos fármacos
Excipientes
Seres Humanos
Microscopia Eletrônica de Varredura
Microesferas
Miocamicina/administração & dosagem
Miocamicina/química
Membrana Mucosa/metabolismo
Soluções Oftálmicas
Tamanho da Partícula
Veias Umbilicais/citologia
Veias Umbilicais/efeitos dos fármacos
Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antiprotozoal Agents); 0 (Excipients); 0 (Ophthalmic Solutions); 059QF0KO0R (Water); 3T48CPS7U2 (Miocamycin); 9012-76-4 (Chitosan); ZPT03UEM0E (rokitamycin)
[Em] Mês de entrada:1002
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090530
[St] Status:MEDLINE
[do] DOI:10.1002/jps.21751


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[PMID]:19403997
[Au] Autor:Fukui M; Nagahara Y; Nishio Y; Honjoh T; Shinomiya T
[Ad] Endereço:Department of Pharmacology, University of Kansas Medical Center, Kansas City, KS 66160, USA.
[Ti] Título:Rokitamycin induces a mitochondrial defect and caspase-dependent apoptosis in human T-cell leukemia Jurkat cells.
[So] Source:J Pharmacol Sci;110(1):69-77, 2009 May.
[Is] ISSN:1347-8613
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Macrolides are a well-known family of oral antibiotics whose antibacterial spectrum of activity covers most relevant bacterial species responsible for respiratory infectious disease. In recent years, it has been reported that macrolides have not only bactericidal activity but also direct immunomodulating activity in mammals. In this study, we observed new physiological activity of macrolides and examined whether various macrolides induce apoptosis in human leukemia cell lines. We investigated the effects of 13 different macrolides on the viability of Jurkat and HL-60 cells. Among all the macrolides used in this study, rokitamycin, a semisynthetic macrolide with a 16-member ring, effectively induced cell death. Rokitamycin induced DNA fragmentation and caspase activation, resembling the progression of apoptosis. Moreover, rokitamycin reduced the mitochondrial transmembrane potential and released cytochrome c from mitochondria to the cytosol, suggesting that mitochondrial perturbation is involved in rokitamycin-induced apoptosis. These results suggest that rokitamycin possesses not only bactericidal activity but also pro-apoptotic activity in human leukemia cells.
[Mh] Termos MeSH primário: Antibacterianos/toxicidade
Apoptose/efeitos dos fármacos
Caspases/fisiologia
Miocamicina/análogos & derivados
Mitocôndrias/efeitos dos fármacos
[Mh] Termos MeSH secundário: Western Blotting
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Citocromos c/metabolismo
Citosol/efeitos dos fármacos
Fragmentação do DNA/efeitos dos fármacos
Relação Dose-Resposta a Droga
Genes p53/fisiologia
Seres Humanos
Proteínas Quinases JNK Ativadas por Mitógeno/metabolismo
Células Jurkat
Macrolídeos/farmacologia
Potenciais da Membrana/efeitos dos fármacos
Miocamicina/toxicidade
Mitocôndrias/ultraestrutura
Membranas Mitocondriais/efeitos dos fármacos
Fosforilação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Macrolides); 3T48CPS7U2 (Miocamycin); 9007-43-6 (Cytochromes c); EC 2.7.11.24 (JNK Mitogen-Activated Protein Kinases); EC 3.4.22.- (Caspases); ZPT03UEM0E (rokitamycin)
[Em] Mês de entrada:0907
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090501
[St] Status:MEDLINE


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[PMID]:18762406
[Au] Autor:Kim JH; Lee YJ; Sohn HJ; Song KJ; Kwon D; Kwon MH; Im KI; Shin HJ
[Ad] Endereço:Department of Microbiology and Department of Molecular Science & Technology, Ajou University School of Medicine, Suwon 443-721, Republic of Korea.
[Ti] Título:Therapeutic effect of rokitamycin in vitro and on experimental meningoencephalitis due to Naegleria fowleri.
[So] Source:Int J Antimicrob Agents;32(5):411-7, 2008 Nov.
[Is] ISSN:0924-8579
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Inhalation of freshwater containing the free-living amoeba Naegleria fowleri leads to a potentially fatal infection known as primary amoebic meningoencephalitis (PAME). Amphotericin B is the only agent with clinical efficacy in the treatment of PAME in humans, however this drug is often associated with adverse effects on the kidney and other organs. In an attempt to select other useful therapeutic agents for treating PAME, the amoebicidal activities of antibacterial agents including clarithromycin, erythromycin, hygromycin B, neomycin, rokitamycin, roxithromycin and zeocin were examined. Results showed that the growth of amoeba was effectively inhibited by treatment with hygromycin B, rokitamycin and roxithromycin. Notably, when N. fowleri trophozoites were treated with rokitamycin, the minimal inhibitory concentration was 6.25 microg/mL on Day 2. In the treatment of experimental meningoencephalitis due to N. fowleri, survival rates of mice treated with roxithromycin and rokitamycin were 25% and 80%, respectively, over 1 month. The mean time to death for roxithromycin and rokitamycin treatment was 16.2 days and 16.8 days, respectively, compared with 11.2 days for control mice. Finally, rokitamycin showed both in vitro and in vivo therapeutic efficacy against N. fowleri and may be a candidate drug for the treatment of PAME.
[Mh] Termos MeSH primário: Amebíase/tratamento farmacológico
Amebicidas/uso terapêutico
Infecções Protozoárias do Sistema Nervoso Central/tratamento farmacológico
Miocamicina/análogos & derivados
Naegleria fowleri
[Mh] Termos MeSH secundário: Amebíase/microbiologia
Amebicidas/farmacologia
Animais
Antibacterianos/uso terapêutico
Nitrogênio da Ureia Sanguínea
Infecções Protozoárias do Sistema Nervoso Central/microbiologia
Feminino
Rim/microbiologia
Rim/patologia
L-Lactato Desidrogenase/metabolismo
Fígado/microbiologia
Fígado/patologia
Camundongos
Camundongos Endogâmicos BALB C
Testes de Sensibilidade Microbiana
Miocamicina/farmacologia
Miocamicina/uso terapêutico
Naegleria fowleri/efeitos dos fármacos
Análise de Sobrevida
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amebicides); 0 (Anti-Bacterial Agents); 3T48CPS7U2 (Miocamycin); EC 1.1.1.27 (L-Lactate Dehydrogenase); ZPT03UEM0E (rokitamycin)
[Em] Mês de entrada:0901
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080903
[St] Status:MEDLINE
[do] DOI:10.1016/j.ijantimicag.2008.05.018


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[PMID]:18329276
[Au] Autor:Furuuchi T; Miura T; Kurihara K; Yoshida T; Watanabe T; Ajito K
[Ad] Endereço:Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama 222-8567, Japan. takeshi_furuuchi@meiji.co.jp
[Ti] Título:Design and synthesis of novel leucomycin analogues modified at the C-3 position. Part II: 3-O-(3-Aryl-2-propenyl)leucomycin analogues.
[So] Source:Bioorg Med Chem;16(8):4401-18, 2008 Apr 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The design and synthesis of 16-membered macrolides modified at the C-3 position are described. Starting from fully protected intermediate (5), appropriate modifications including Heck reaction were performed to furnish 3-O-(3-aryl-2-propenyl)leucomycin A(7) analogues (9a-9m). These leucomycin A(7) derivatives showed improved in vitro antibacterial activities against clinically important pathogens including erythromycin-resistant Streptococcus pneumoniae (ERSP). SAR analysis of derivatives modified at the C-3 and C-3'' positions suggested that single modification at C-3 or C-3'' was effective for in vitro antibacterial activity.
[Mh] Termos MeSH primário: Antibacterianos/síntese química
Antibacterianos/farmacologia
Desenho de Drogas
Kitasamicina/síntese química
Kitasamicina/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/química
Benzoquinonas/química
Cristalografia por Raios X
Kitasamicina/análogos & derivados
Kitasamicina/química
Miocamicina/análogos & derivados
Miocamicina/síntese química
Miocamicina/química
Miocamicina/farmacologia
Modelos Moleculares
Estrutura Molecular
Streptococcus/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Benzoquinones); 1392-21-8 (Kitasamycin); 3T006GV98U (quinone); 3T48CPS7U2 (Miocamycin); ZPT03UEM0E (rokitamycin)
[Em] Mês de entrada:0805
[Cu] Atualização por classe:161124
[Lr] Data última revisão:
161124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080311
[St] Status:MEDLINE
[do] DOI:10.1016/j.bmc.2008.02.064


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[PMID]:18258437
[Au] Autor:Miura T; Kurihara K; Furuuchi T; Yoshida T; Ajito K
[Ad] Endereço:Pharmaceutical Research Center, Meiji Seika Kaisha Ltd, 760 Morooka-cho, Kohoku-ku, Yokohama 222-8567, Japan. tomoaki_miura@meiji.co.jp
[Ti] Título:Novel 16-membered macrolides modified at C-12 and C-13 positions of midecamycin A1 and miokamycin. Part 1: Synthesis and evaluation of 12,13-carbamate and 12-arylalkylamino-13-hydroxy analogues.
[So] Source:Bioorg Med Chem;16(7):3985-4002, 2008 Apr 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Design and synthesis of 16-membered macrolides modified at the C-12 and 13 positions are described. The compounds we report here have an arylalkylamino group attached to the C-12 position of the macrolactone. Both types of derivatives, 12,13-cyclic carbamates and non-carbamate analogues, were synthesized via 12-amino-13-hydroxy intermediates derived from 12,13-epoxide that was prepared by selective epoxidation at the C-12 and C-13 positions. 4'-Hydroxyl analogues were also prepared by acidic hydrolysis of a neutral sugar. These compounds were evaluated for in vitro antibacterial activity against respiratory tract pathogens. Some of these analogues exhibited an improved activity compared with the corresponding parent compound.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Carbamatos/síntese química
Carbamatos/farmacologia
Leucomicinas/síntese química
Leucomicinas/farmacologia
Miocamicina/síntese química
Miocamicina/farmacologia
[Mh] Termos MeSH secundário: Alquilação
Aminação
Antibacterianos/síntese química
Antibacterianos/química
Carbamatos/química
Hidroxilação
Cetolídeos/química
Leucomicinas/química
Viabilidade Microbiana/efeitos dos fármacos
Miocamicina/química
Estrutura Molecular
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Carbamates); 0 (Ketolides); 0 (Leucomycins); 3T48CPS7U2 (Miocamycin); N34Z0Y5UH7 (midecamycin)
[Em] Mês de entrada:0805
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080209
[St] Status:MEDLINE
[do] DOI:10.1016/j.bmc.2008.01.027


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[PMID]:18082375
[Au] Autor:Roveta S; Marchese A; Debbia EA; Bandettini R
[Ti] Título:In vitro synergism between rokitamycin and co-trimoxazole against Streptococcus pyogenes, Streptococcus pneumoniae and staphylococci.
[So] Source:Int J Antimicrob Agents;31(2):185-7, 2008 Feb.
[Is] ISSN:0924-8579
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Sinergismo Farmacológico
Streptococcus pneumoniae/efeitos dos fármacos
Streptococcus pyogenes/efeitos dos fármacos
[Mh] Termos MeSH secundário: Combinação de Medicamentos
Farmacorresistência Bacteriana
Testes de Sensibilidade Microbiana
Miocamicina/análogos & derivados
Miocamicina/farmacologia
Streptococcus pneumoniae/crescimento & desenvolvimento
Streptococcus pyogenes/crescimento & desenvolvimento
Combinação Trimetoprima e Sulfametoxazol/farmacologia
[Pt] Tipo de publicação:LETTER
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Drug Combinations); 3T48CPS7U2 (Miocamycin); 8064-90-2 (Trimethoprim, Sulfamethoxazole Drug Combination); ZPT03UEM0E (rokitamycin)
[Em] Mês de entrada:0806
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:071218
[St] Status:MEDLINE



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