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[PMID]:28356898
[Au] Autor:Lu LJ; Tsai JC; Liu J
[Ad] Endereço:Department of Ophthalmology and Visual Science, Yale School of Medicine, New Haven, Connecticut.
[Ti] Título:Novel Pharmacologic Candidates for Treatment of Primary Open-Angle Glaucoma.
[So] Source:Yale J Biol Med;90(1):111-118, 2017 Mar.
[Is] ISSN:1551-4056
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Primary open-angle glaucoma (OAG) affects approximately 45 million people worldwide and more than 2.5 million people aged 40 years or older in the United States. Pharmacologic treatment for glaucoma is directed towards lowering intraocular pressure (IOP) to slow disease progression and delay visual field loss. Current medical treatment options for the lowering of IOP include the following classes of topical medications: beta-adrenergic antagonists, alpha-adrenergic agonists, cholinergic agonists, carbonic anhydrase inhibitors, and prostaglandin analogs. Issues with existing drugs include failure to achieve target IOP with monotherapy, drug-related side effects, and low patient compliance with multiple daily administration of eye drops. In recent years, the scientific and medical community has seen encouraging development of novel classes of drugs for primary OAG, the majority of which lower IOP by targeting the trabecular meshwork outflow pathway to increase aqueous humor outflow. Among the most promising new pharmacologic candidates are rho kinase inhibitors including ripasudil (K-115), netarsudil (AR-13324), and AMA0076; adenosine receptor agonists including trabodenoson (INO-8875); and modified prostaglandin analogs including latanoprostene bunod (LBN, BOL-303259-X) and ONO-9054. This study aims to systematically review and summarize the most recent developments in clinical trials for new pharmacologic options for the treatment of primary open-angle glaucoma.
[Mh] Termos MeSH primário: Glaucoma de Ângulo Aberto/tratamento farmacológico
[Mh] Termos MeSH secundário: Glaucoma de Ângulo Aberto/enzimologia
Seres Humanos
Pressão Intraocular/efeitos dos fármacos
Isoquinolinas/uso terapêutico
Oxepinas/uso terapêutico
Prostaglandinas F Sintéticas/uso terapêutico
Sulfonamidas/uso terapêutico
Quinases Associadas a rho/antagonistas & inibidores
Quinases Associadas a rho/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (BOL 303259-X); 0 (Isoquinolines); 0 (K-115); 0 (Oxepins); 0 (Prostaglandins F, Synthetic); 0 (Sulfonamides); 0 (propan-2-yl 4-(6-(4-(2,5-difluorophenoxy)-3-hydroxybut-1-en-1-yl)-7-hydroxyoctahydro-2H-cyclopenta(b)oxepin-3-yl)butanoate); EC 2.7.11.1 (rho-Associated Kinases)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170331
[St] Status:MEDLINE


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[PMID]:27649982
[Au] Autor:Miller Ellis E; Berlin MS; Ward CL; Sharpe JA; Jamil A; Harris A
[Ad] Endereço:Perelman School of Medicine at the University of Pennsylvania, Philadelphia, Pennsylvania, USA.
[Ti] Título:Ocular hypotensive effect of the novel EP3/FP agonist ONO-9054 versus Xalatan: results of a 28-day, double-masked, randomised study.
[So] Source:Br J Ophthalmol;101(6):796-800, 2017 Jun.
[Is] ISSN:1468-2079
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIMS: ONO-9054 is being developed for the reduction of intraocular pressure (IOP) in patients with ocular hypertension (OHT) and open-angle glaucoma (OAG). This study compared the novel dual EP3/FP agonist ONO-9054 with the FP agonist Xalatan. METHODS: Adults (n=123) with bilateral mild/moderate OAG or OHT, with unmedicated IOP of ≥24 mm Hg at 8:00 hours, ≥21 mm Hg at 10:00 hours and ≤36 mm Hg, were randomised 1:1 to receive ONO-9054 (0.003%, 30 µg/mL) or Xalatan (0.005%, 50 µg/mL) once daily for 28 days. RESULTS: Day 29 mean diurnal IOP was -7.2 mm Hg for ONO-9054 vs -6.6 mm Hg for Xalatan. At 08:00 hours, the IOPs were comparable, and at all later time points the decrease in IOP was greater for ONO-9054. On day 29, the odds of a mean IOP reduction of ≤-25%, ≤-30% and ≤-35% for ONO-9054 were 2.39, 2.37 and 4.85 times more, respectively, than the odds for Xalatan (p<0.05, analyses). The percentage of subjects achieving target IOPs on day 29 (≤17, ≤16 and ≤15 mm Hg) was greater for ONO-9054 than for Xalatan; the odds of achieving an IOP ≤15 mm Hg for ONO-9054 were 2.4 times more than the odds for Xalatan (p<0.01, analysis). CONCLUSIONS: Subjects randomised to receive ONO-9054 were more likely to achieve a greater per cent reduction in IOP and were more likely to achieve target IOPs than those receiving Xalatan. The effects of ONO-9054 in reducing IOP appear to persist longer than those of Xalatan. TRIAL REGISTRATION NUMBER: NCT02083289, Results.
[Mh] Termos MeSH primário: Glaucoma de Ângulo Aberto/tratamento farmacológico
Pressão Intraocular/efeitos dos fármacos
Hipertensão Ocular/tratamento farmacológico
Oxepinas/administração & dosagem
Prostaglandinas F Sintéticas/administração & dosagem
[Mh] Termos MeSH secundário: Adolescente
Adulto
Idoso
Idoso de 80 Anos ou mais
Relação Dose-Resposta a Droga
Método Duplo-Cego
Feminino
Seguimentos
Glaucoma de Ângulo Aberto/fisiopatologia
Seres Humanos
Masculino
Meia-Idade
Hipertensão Ocular/fisiopatologia
Soluções Oftálmicas
Estudos Retrospectivos
Fatores de Tempo
Resultado do Tratamento
Adulto Jovem
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE II; JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Ophthalmic Solutions); 0 (Oxepins); 0 (Prostaglandins F, Synthetic); 0 (propan-2-yl 4-(6-(4-(2,5-difluorophenoxy)-3-hydroxybut-1-en-1-yl)-7-hydroxyoctahydro-2H-cyclopenta(b)oxepin-3-yl)butanoate); 6Z5B6HVF6O (latanoprost)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170910
[Lr] Data última revisão:
170910
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160922
[St] Status:MEDLINE
[do] DOI:10.1136/bjophthalmol-2016-309023


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[PMID]:27745908
[Au] Autor:Chepkirui C; Richter C; Matasyoh JC; Stadler M
[Ad] Endereço:Helmholtz Centre for Infection Research GmbH (HZI), Department Microbial Drugs, Inhoffenstraße 7, 38124, Braunschweig, Germany.
[Ti] Título:Monochlorinated calocerins A-D and 9-oxostrobilurin derivatives from the basidiomycete Favolaschia calocera.
[So] Source:Phytochemistry;132:95-101, 2016 Dec.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Eight previously undescribed compounds were isolated and characterised from the supernatant and mycelium of a culture of the basidiomycete Favolaschia calocera originating from Kakamega equatorial rainforest in Kenya. These were: 9- oxostrobilurins A, G, K and I and the four monochlorinated calocerins A, B, C and D. The calocerins extend our knowledge of halogenated compounds obtained from natural sources. Four further known compounds were also identified: strobilurin G, favolon, pterulinic acid and 2,3 -dihydro-1-benzoxepin derivative. The four oxostrobilurins exhibited prominent antifungal and cytotoxic activities while the four calocerins only showed cytotoxic activity.
[Mh] Termos MeSH primário: Antifúngicos/isolamento & purificação
Basidiomycota/química
Ácidos Graxos Insaturados/isolamento & purificação
Hidrocarbonetos Clorados/isolamento & purificação
Metacrilatos/isolamento & purificação
[Mh] Termos MeSH secundário: Antifúngicos/química
Antifúngicos/farmacologia
Benzofuranos/química
Ensaios de Seleção de Medicamentos Antitumorais
Ácidos Graxos Insaturados/química
Ácidos Graxos Insaturados/farmacologia
Seres Humanos
Hidrocarbonetos Clorados/química
Hidrocarbonetos Clorados/farmacologia
Quênia
Metacrilatos/química
Metacrilatos/farmacologia
Testes de Sensibilidade Microbiana
Oxepinas/química
Estrobilurinas
Triterpenos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antifungal Agents); 0 (Benzofurans); 0 (Fatty Acids, Unsaturated); 0 (Hydrocarbons, Chlorinated); 0 (Methacrylates); 0 (Oxepins); 0 (Strobilurins); 0 (Triterpenes); 0 (favolon); 0 (pterulinic acid); 49G3784VEO (strobilurin G)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161018
[St] Status:MEDLINE


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[PMID]:27692326
[Au] Autor:Sales N; Love S
[Ad] Endereço:NSW DPI, Elizabeth Macarthur Agricultural Institute, Private Bag 4008, Narellan, NSW 2567, Australia. Electronic address: narelle.sales@dpi.nsw.gov.au.
[Ti] Título:Resistance of Haemonchus sp. to monepantel and reduced efficacy of a derquantel / abamectin combination confirmed in sheep in NSW, Australia.
[So] Source:Vet Parasitol;228:193-196, 2016 Sep 15.
[Is] ISSN:1873-2550
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Early in 2015, sheep in a summer rainfall area of NSW, Australia, displayed signs of haemonchosis despite treatment with monepantel. A faecal egg count reduction test (FECRT) was performed on yearlings with natural field infections using various anthelmintics. Only a four-way combination drench achieved a reduction in faecal egg count (FEC) greater than 95%. The combination contained abamectin, albendazole, levamisole and closantel. Treatments with a derquantel/abamectin combination, monepantel and moxidectin reduced FECs by 93, 31, and 30% respectively. Sheep treated with abamectin displayed an increase in FEC of 22%. Larval differentiation counts conducted 10days post-treatment showed that 100% of survivors were Haemonchus sp. This result confirms for the first time monepantel resistant Haemonchus in sheep in NSW, and is amongst the first of the Australian cases in sheep not associated with goats. A second FECRT was performed using sheep from the moxidectin and abamectin treatment groups in the first FECRT. In this second FECRT, monepantel treatment reduced FECs by 51% and 29% in the sheep previously treated with moxidectin and abamectin respectively. This suggests monepantel, in combination with moxidectin, may give some control against severely abamectin resistant Haemonchus.
[Mh] Termos MeSH primário: Aminoacetonitrila/análogos & derivados
Anti-Helmínticos/farmacologia
Hemoncose/veterinária
Haemonchus/efeitos dos fármacos
Doenças dos Ovinos/parasitologia
[Mh] Termos MeSH secundário: Albendazol/farmacologia
Aminoacetonitrila/farmacologia
Animais
Austrália
Quimioterapia Combinada
Fezes/parasitologia
Hemoncose/tratamento farmacológico
Hemoncose/parasitologia
Indóis/farmacologia
Ivermectina/análogos & derivados
Ivermectina/farmacologia
Macrolídeos/farmacologia
Masculino
Oxepinas/farmacologia
Contagem de Ovos de Parasitas/veterinária
Distribuição Aleatória
Salicilanilidas/farmacologia
Ovinos
Doenças dos Ovinos/tratamento farmacológico
Falha de Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Indoles); 0 (Macrolides); 0 (Oxepins); 0 (Salicylanilides); 0L0UGK6OOX (derquantel); 3739OQ10IJ (Aminoacetonitrile); 51570-36-6 (milbemycin); 5U8924T11H (abamectin); 70288-86-7 (Ivermectin); 82MA79VJ33 (monepantel); EUL532EI54 (closantel); F4216019LN (Albendazole)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170807
[Lr] Data última revisão:
170807
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161004
[St] Status:MEDLINE


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[PMID]:27617983
[Au] Autor:Sun TY; Kuang RQ; Chen GD; Qin SY; Wang CX; Hu D; Wu B; Liu XZ; Yao XS; Gao H
[Ad] Endereço:Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, China. sty4048588@163.com.
[Ti] Título:Three Pairs of New Isopentenyl Dibenzo[b,e]oxepinone Enantiomers from Talaromyces flavus, a Wetland Soil-Derived Fungus.
[So] Source:Molecules;21(9), 2016 Sep 07.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Three pairs of new isopentenyl dibenzo[b,e]oxepinone enantiomers, (+)-(5S)-arugosin K (1a), (-)-(5R)-arugosin K (1b), (+)-(5S)-arugosin L (2a), (-)-(5R)-arugosin L (2b), (+)-(5S)-arugosin M (3a), (-)-(5R)-arugosin M (3b), and a new isopentenyl dibenzo[b,e]oxepinone, arugosin N (4), were isolated from a wetland soil-derived fungus Talaromyces flavus, along with two known biosynthetically-related compounds 5 and 6. Among them, arugosin N (4) and 1,6,10-trihydroxy-8-methyl-2-(3-methyl-2-butenyl)-dibenz[b,e]oxepin-11(6H)-one (CAS: 160585-91-1, 5) were obtained as the tautomeric mixtures. The structures of isolated compounds were determined by detailed spectroscopic analysis. In addition, the absolute configurations of these three pairs of new enantiomers were determined by quantum chemical ECD calculations.
[Mh] Termos MeSH primário: Oxepinas
Microbiologia do Solo
Talaromyces/química
[Mh] Termos MeSH secundário: Oxepinas/química
Oxepinas/isolamento & purificação
Zonas Úmidas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Oxepins)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170417
[Lr] Data última revisão:
170417
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160913
[St] Status:MEDLINE


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[PMID]:27513663
[Au] Autor:Snider NT; Portney DA; Willcockson HH; Maitra D; Martin HC; Greenson JK; Omary MB
[Ad] Endereço:Department of Cell Biology and Physiology, University of North Carolina, Chapel Hill, NC, 27599, United States of America.
[Ti] Título:Ethanol and Acetaminophen Synergistically Induce Hepatic Aggregation and TCH346-Insensitive Nuclear Translocation of GAPDH.
[So] Source:PLoS One;11(8):e0160982, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The glycolytic enzyme glyceraldehyde-3-phosphate dehydrogenase (GAPDH) signals during cellular stress via several post-translational modifications that change its folding properties, protein-protein interactions and sub-cellular localization. We examined GAPDH properties in acute mouse liver injury due to ethanol and/or acetaminophen (APAP) treatment. Synergistic robust and time-dependent nuclear accumulation and aggregation of GAPDH were observed only in combined, but not individual, ethanol/APAP treatments. The small molecule GAPDH-targeting compound TCH346 partially attenuated liver damage possibly via mitochondrial mechanisms, and independent of nuclear accumulation and aggregation of GAPDH. These findings provide a novel potential mechanism for hepatotoxicity caused by combined alcohol and acetaminophen exposure.
[Mh] Termos MeSH primário: Acetaminofen/toxicidade
Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico
Etanol/toxicidade
Gliceraldeído-3-Fosfato Desidrogenases/metabolismo
Fígado/efeitos dos fármacos
Oxepinas/farmacologia
Transporte Proteico/efeitos dos fármacos
[Mh] Termos MeSH secundário: Analgésicos não Entorpecentes/toxicidade
Animais
Núcleo Celular/metabolismo
Depressores do Sistema Nervoso Central/toxicidade
Sinergismo Farmacológico
Feminino
Fígado/metabolismo
Camundongos
Camundongos Endogâmicos C57BL
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics, Non-Narcotic); 0 (Central Nervous System Depressants); 0 (Oxepins); 0 (dibenzo(b,f)oxepin-10-ylmethyl-methyl-prop-2-ynyl-amine); 362O9ITL9D (Acetaminophen); 3K9958V90M (Ethanol); EC 1.2.1.- (Glyceraldehyde-3-Phosphate Dehydrogenases)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170803
[Lr] Data última revisão:
170803
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160812
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0160982


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[PMID]:27405218
[Au] Autor:Dzhafarov MKh; Vasilevich F; Dovgalev AS; Imamkuliev KD; Pautova EA
[Ti] Título:[ANTHELMINTIC SUBSTANCES: MAIN CLASSES, PROBLEMS, TRENDS IN DEVELOPMENT AND PROSPECTS].
[So] Source:Med Parazitol (Mosk);(2):47-53, 2016 Apr-Jun.
[Is] ISSN:0025-8326
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The review chronologically considers the main classes of the currently available anthelminthic substances: early anthelmintic compounds, benzimidazoles, imidazolthiazoles, tetrahydropyrimidines, avermectins and milbemycins, and salicylanilides. Great attention is paid to novel substances (emodepside, monepantel, derquantel, tribendimidine) and promising developments. Some aspects of the molecular mechanisms of action of anthelmintics, their resistance, and alternative dehelmintization methods are discussed.
[Mh] Termos MeSH primário: Anti-Helmínticos/classificação
Cestoides/efeitos dos fármacos
Desenho de Drogas
Nematoides/efeitos dos fármacos
Trematódeos/efeitos dos fármacos
[Mh] Termos MeSH secundário: Aminoacetonitrila/análogos & derivados
Aminoacetonitrila/síntese química
Aminoacetonitrila/farmacologia
Animais
Anti-Helmínticos/síntese química
Anti-Helmínticos/farmacologia
Produtos Biológicos/química
Produtos Biológicos/farmacologia
Cestoides/fisiologia
Infecções por Cestoides/diagnóstico
Infecções por Cestoides/tratamento farmacológico
Infecções por Cestoides/parasitologia
Depsipeptídeos/síntese química
Depsipeptídeos/farmacologia
Seres Humanos
Indóis/síntese química
Indóis/farmacologia
Medicina Tradicional
Nematoides/fisiologia
Infecções por Nematoides/diagnóstico
Infecções por Nematoides/tratamento farmacológico
Infecções por Nematoides/parasitologia
Oxepinas/síntese química
Oxepinas/farmacologia
Fenilenodiaminas/síntese química
Fenilenodiaminas/farmacologia
Trematódeos/fisiologia
Infecções por Trematódeos/diagnóstico
Infecções por Trematódeos/tratamento farmacológico
Infecções por Trematódeos/parasitologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anthelmintics); 0 (Biological Products); 0 (Depsipeptides); 0 (Indoles); 0 (Oxepins); 0 (Phenylenediamines); 0L0UGK6OOX (derquantel); 115103-15-6 (tribendimidine); 3739OQ10IJ (Aminoacetonitrile); 82MA79VJ33 (monepantel); YZ647Y5GC9 (emodepside)
[Em] Mês de entrada:1607
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160714
[St] Status:MEDLINE


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[PMID]:27300645
[Au] Autor:Harris A; Ward CL; Rowe-Rendleman CL; Ouchi T; Wood A; Fujii A; Serle JB
[Ad] Endereço:*Indiana University School of Medicine, Indianapolis, IN †Ono Pharma UK Ltd, London, UK ‡Omar Consulting Group LLC, Princeton Junction §Ono Pharma USA, Lawrenceville, NJ ∥Icahn School of Medicine at Mount Sinai, Mount Sinai Hospital, New York, NY.
[Ti] Título:Ocular Hypotensive Effect of ONO-9054, an EP3/FP Receptor Agonist: Results of a Randomized, Placebo-controlled, Dose Escalation Study.
[So] Source:J Glaucoma;25(10):e826-e833, 2016 Oct.
[Is] ISSN:1536-481X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: To assess pharmacodynamic and safety profiles of ONO-9054 following single and multiple day dosing in subjects with ocular hypertension or open-angle glaucoma. MATERIALS AND METHODS: This was a phase I, single-center, randomized, double-masked, placebo-controlled dose-escalation study. Nine subjects were randomized to each of ONO-9054 3, 10, 20, 30 µg/mL and 12 to placebo. Subjects received a single drop to each eye at 07:00±30 minutes (single dose). Following a 4-day no-treatment period, subjects were dosed once daily for 14 consecutive days (multiple day dosing). Intraocular pressure (IOP) was measured regularly and compared with baseline measurements. Ocular examinations assessed safety and tolerability. RESULTS: Mean IOP decreased dose dependently. Following single dosing, IOP decreased from 22.9±4.0 to 15.9±2.3 mm Hg (ONO-9054, 30 µg/mL) at peak effect 9 hours postdose; the reduction in placebo-treated subjects was from 22.3±2.4 to 21.5±3.3 mm Hg. Following multiple day dosing, the greatest reduction in IOP occurred 1 hour postdose on day 18, from 23.3±0.6 to 15.1±2.4 mm Hg (ONO-9054, 10 µg/mL); the smallest reduction at this time was from 23.9±0.8 to 18.6±2.0 mm Hg (ONO-9054, 3 µg/mL). Pressures remained reduced on day 19, 25 hours after the last dose, when the lowest measurement was 15.8±2.1 mm Hg (ONO-9054, 10 µg/mL). Anterior uveitis and vitreous detachment were each reported in 2 subjects and considered moderate by the Investigator. Ocular hyperemia and tolerability symptoms were generally mild and transient. CONCLUSIONS: ONO-9054 was well-tolerated and elicited dose-dependent reductions in IOP, which were sustained for at least 24 hours following 2 weeks of consecutive daily dosing.
[Mh] Termos MeSH primário: Anti-Hipertensivos/uso terapêutico
Glaucoma de Ângulo Aberto/tratamento farmacológico
Pressão Intraocular/efeitos dos fármacos
Hipertensão Ocular/tratamento farmacológico
Oxepinas/uso terapêutico
Receptores de Prostaglandina/antagonistas & inibidores
[Mh] Termos MeSH secundário: Idoso
Anti-Hipertensivos/farmacologia
Relação Dose-Resposta a Droga
Método Duplo-Cego
Feminino
Seres Humanos
Masculino
Meia-Idade
Oxepinas/farmacologia
Tonometria Ocular
[Pt] Tipo de publicação:CLINICAL TRIAL, PHASE I; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Antihypertensive Agents); 0 (Oxepins); 0 (Receptors, Prostaglandin); 0 (propan-2-yl 4-(6-(4-(2,5-difluorophenoxy)-3-hydroxybut-1-en-1-yl)-7-hydroxyoctahydro-2H-cyclopenta(b)oxepin-3-yl)butanoate); 0 (prostaglandin F2alpha receptor)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160615
[St] Status:MEDLINE


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[PMID]:27056249
[Au] Autor:Vannam R; Peczuh MW
[Ad] Endereço:Department of Chemistry, University of Connecticut, 55 North Eagleville Road, U-3060, Storrs, CT 06269, USA. mark.peczuh@uconn.edu.
[Ti] Título:A practical and scalable synthesis of carbohydrate based oxepines.
[So] Source:Org Biomol Chem;14(16):3989-96, 2016 Apr 28.
[Is] ISSN:1477-0539
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:An efficient, seven-step synthesis of carbohydrate based oxepines is reported using per-O-acetyl septanoses as key intermediates. The scope of the synthesis was evaluated by varying both the pyranose starting materials and protecting groups incorporated into the oxepine products. The practicality of the method make it amenable to scale up as demonstrated by the gram-scale synthesis of the d-glucose derived oxepine.
[Mh] Termos MeSH primário: Carboidratos/química
Dioxolanos/química
Cetonas/química
Oxepinas/síntese química
[Mh] Termos MeSH secundário: Catálise
Cristalografia por Raios X
Espectroscopia de Ressonância Magnética
Estrutura Molecular
Oxepinas/química
Espectrometria de Massas por Ionização por Electrospray
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Carbohydrates); 0 (Dioxolanes); 0 (Ketones); 0 (Oxepins)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160409
[St] Status:MEDLINE
[do] DOI:10.1039/c6ob00262e


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[PMID]:26998701
[Au] Autor:Wang J; He W; Huang X; Tian X; Liao S; Yang B; Wang F; Zhou X; Liu Y
[Ad] Endereço:CAS Key Laboratory of Tropical Marine Bio-resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences , Guangzhou 510301, People's Republic of China.
[Ti] Título:Antifungal New Oxepine-Containing Alkaloids and Xanthones from the Deep-Sea-Derived Fungus Aspergillus versicolor SCSIO 05879.
[So] Source:J Agric Food Chem;64(14):2910-6, 2016 Apr 13.
[Is] ISSN:1520-5118
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Phytopathogenic fungi remain a continuous and huge threat in the agricultural fields. The agrochemical industry has made great development of the use of microbial natural products, which has been regarded as an effective strategy against phytopathogenic fungi. Antifungal bioassay-directed fractionation was used to isolate two new oxepine-containing alkaloids (1 and 2), two new 4-aryl-quinolin-2-one alkaloids (3 and 4), and four new prenylated xanthones (5-8) from the deep-sea-derived fungus Aspergillus versicolor SCSIO 05879. Extensive NMR spectroscopic analysis, quantum mechanical calculations, and X-ray single-crystal diffraction were used to elucidate their structures, including their absolute configurations. Versicoloids A and B, versicone A, and cottoquinazoline A showed antifungal activities against three phytopathogenic fungi. The antifungal activities of these bioactive compounds strongly depend on the fungal species. Especially versicoloids A and B showed strong fungicidal effect (MIC of 1.6 µg/mL) against Colletotrichum acutatum, compared with that of the positive control cycloheximide (MIC of 6.4 µg/mL). The results of antifungal experiments indicated that versicoloids A and B may be regarded as candidate agents of antifungal agrochemicals.
[Mh] Termos MeSH primário: Alcaloides/farmacologia
Aspergillus/química
Fungicidas Industriais/farmacologia
Água do Mar/microbiologia
Xantonas/farmacologia
[Mh] Termos MeSH secundário: Alcaloides/química
Aspergillus/isolamento & purificação
Colletotrichum/efeitos dos fármacos
Fungicidas Industriais/química
Testes de Sensibilidade Microbiana
Estrutura Molecular
Oxepinas/análise
Oxepinas/química
Xantonas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Alkaloids); 0 (Fungicides, Industrial); 0 (Oxepins); 0 (Xanthones)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160322
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jafc.6b00527



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