965 resultados para N-methoxy-N-methyl-2-[(4 ` substituted)phenylsulfinyl]propanamides


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Two new chromenols, namely (R)-2-methyl-2-(4-methylpenta-1,3-dienyl)-2H-chromen-6-ol (7) and 1-[(R)-6-hydroxy-2-methyl-2H-chromen-2-yl]-4-methylpentan-2-one (8), have been isolated from a southern Australian tunicate, Aplidium solidum. The structures of (7) and (8) were assigned by spectroscopic analysis, and the absolute stereochemistry of (7) by chemical degradation.

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BACKGROUND: Congenital diaphragmatic hernia (CDH) is associated with pulmonary hypertension and death. Administration of nitric oxide (NO) alone remains ineffective in CDH cases. We investigated in near full-term lambs with and without CDH the role of guanylate cyclase (GC), the enzyme activated by NO in increasing cyclic 3'-5'-guanylosine monophosphate, and the role of phosphodiesterase (PDE) 5, the enzyme-degrading cyclic 3'-5'-guanylosine monophosphate. METHODS: Congenital diaphragmatic hernia was surgically created in fetal lambs at 85 days of gestation. Pulmonary hemodynamics were assessed by means of pressure and blood flow catheters (135 days). In vitro, we tested drugs on rings of isolated pulmonary vessels. RESULTS: In vivo, sodium nitroprusside, a direct NO donor, and methyl-2(4-aminophenyl)-1,2-dihydro-1-oxo-7-(2-pyridinylmethoxy)-4-(3,4,5 trimethoxyphenyl)-3-isoquinoline carboxylate sulfate (T-1032) and Zaprinast, both PDE 5 blockers, reduced pulmonary vascular resistance in CDH and non-CDH animals. The activation of GC by sodium nitroprusside and the inhibition of PDE 5 by T-1032 were less effective in CDH animals. In vitro, the stimulation of GC by 3(5'hydroxymethyl-2'furyl)-1-benzyl indazole (YC-1) (a benzyl indazole derivative) and the inhibition of PDE 5 by T-1032 were less effective in pulmonary vascular rings from CDH animals. The YC-1-induced vasodilation in rings from CDH animals was higher when associated with the PDE 5 inhibitor T-1032. CONCLUSIONS: Guanylate cyclase and PDE 5 play a role in controlling pulmonary vascular tone in fetal lambs with or without CDH. Both enzymes seem to be impaired in fetal lambs with CDH.

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Foram conduzidos quatro experimentos de campo, sendo dois no município de Santo Antônio de Goiás-GO e dois no município de Santa Helena de Goiás-GO, nos anos agrícolas de 1998/1999 e 1999/2000, com o objetivo de avaliar a seletividade de herbicidas para a cultura do arroz de terras altas em diferentes estádios da planta, dos cultivares Maravilha, Primavera e Canastra. Os tratamentos foram: metsulfuron-methyl (2,4 g i.a. ha-1) aos 10 e 20 dias após a emergência (DAE); 2,4-D amina (335, 502 e 670 g i.a ha-1) aos 10, 20 e 30 DAE; fenoxaprop-p-ethyl (41,4 g i.a. ha-1) aos 10, 20 e 30 DAE; e clefoxydin (120 g i.a. ha¹) aos 10, 20 e 30 DAE. A seletividade dos herbicidas dependeu do cultivar e do estádio de desenvolvimento da planta do arroz. Assim, os resultados permitem concluir que é recomendada para o cultivar Primavera a aplicação de metsulfuron-methyl aos 20 DAE e de fenoxaprop-p-ethyl e clefoxydin aos 30 DAE; o herbicida 2,4-D amina não é recomendado para este cultivar. Para o cultivar Maravilha, o metsulfuron-methyl e o fenoxaprop-p-ethyl podem ser aplicados em qualquer estádio do crescimento. Os herbicidas 2,4-D amina e clefoxydin são recomendados para aplicação aos 30 DAE. O cultivar Canastra apresentou alta resistência à aplicação dos herbicidas em todos os estádios de crescimento analisados.

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Objetivou-se neste trabalho avaliar a seletividade de herbicidas aplicados nas gramas Santo Agostinho (Stenotaphrum secundatum) e Esmeralda (Zoysia japonica) em condições de campo. O delineamento experimental utilizado foi o de blocos casualizados, com quatro repetições. As gramas foram cortadas a 3 cm de altura e, em seguida, foram feitas as aplicações dos herbicidas. Os tratamentos utilizados foram: testemunha sem aplicação, fluazifop-p-butil (125 g ha-1), sethoxydim+óleo mineral (276 g ha-1 + 0,5% v v-1 de Assist), bispyribac-sodium (25 g ha-1), chlorimuron-ethyl (15 g ha-1), ethoxysulfuron (150 g ha-1), halosulfuron (112,5 g ha-1), iodosulfuron-methyl (10 g ha-1), metsulfuron-methyl (2,4 g ha-1), nicosulfuron (125 g ha-1), pyrithiobac-sodium (140 g ha-1), trifloxysulfuron-sodium (22,5 g ha-1), 2,4-D (720 g ha-1), quinclorac (375 g ha-1), atrazina (1.250 g ha-1), bentazon (600 g ha-1), linuron (1.350 g ha-1), fomesafen (187,5 g ha-1), lactofen (120 g ha-1), oxadiazon (600 g ha-1) e oxyfluorfen (720 g ha-1). Os herbicidas que apresentaram potencial de seletividade para o gramado de S. secundatum foram: os inibidores da ALS chlorimuron-ethyl, ethoxysulfuron, halosulfuron, iodosulfuron-methyl e metsulfuron-methyl, o mimetizador de auxina 2,4-D, os inibidores do fotossistema II atrazina e bentazon, bem como os inibidores da Protox fomesafen, lactofen e o oxadiazon. Para o gramado de Z. japonica, os herbicidas que apresentaram potencial de seletividade foram: os inibidores da ALS chlorimuron-ethyl, ethoxysulfuron, halosulfuron, metsulfuron-methyl e nicosulfuron, os mimetizadores de auxina 2,4-D e quinclorac, os inibidores do fotossistema II atrazina e bentazon, além dos inibidores da Protox fomesafen, lactofen e o oxadiazon.

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Objetivou-se avaliar a seletividade de herbicidas aplicados na grama Batatais (Paspalum notatum) e na grama São Carlos (Axonopus compressus) em campo. O delineamento experimental utilizado foi o de blocos casualizados com quatro repetições. As gramas foram cortadas a 3 cm de altura e, em seguida, realizaram-se as aplicações dos herbicidas. Os tratamentos utilizados foram: testemunha (sem aplicação), fluazifop-p-butil (125 g ha-1), sethoxydim+óleo mineral (276 g ha-1 + 0,5% v v-1 de Assist), bispyribac-sodium (25 g ha-1), chlorimuron-ethyl (15 g ha-1), ethoxysulfuron (150 g ha-1), halosulfuron (112,5 g ha-1), iodosulfuron-methyl (10 g ha-1), metsulfuron-methyl (2,4 g ha-1), nicosulfuron (125 g ha-1), pyrithiobac-sodium (140 g ha-1), trifloxysulfuron-sodium (22,5 g ha-1), 2,4-D (720 g ha-1), quinclorac (375 g ha-1), atrazina (1.250 g ha-1), bentazon (600 g ha-1), linuron (1.350 g ha-1), fomesafen (187,5 g ha-1), lactofen (120 g ha-1), oxadiazon (600 g ha-1) e oxyfluorfen (720 g ha-1). Os herbicidas que apresentaram potencial de seletividade para o gramado de P. notatum foram o chlorimuron-ethyl, ethoxysulfuron, pyrithiobac-sodium, 2,4-D, bentazon e fomesafen; já para o gramado de A. compressus foram o chlorimuron-ethyl, ethoxysulfuron, halosulfuron, iodosulfuron-methyl, metsulfuron-methyl, pyrithiobac-sodium, 2,4-D, quinclorac, atrazina, bentazon, além do fomesafen.

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In eukaryotes, wobble uridines in the anticodons of tRNALysUUU, tRNAGluUUC and tRNAGlnUUG are modified to 5-methoxy-carbonyl-methyl-2-thio-uridine (mcm5s2U). While mutations in subunits of the Elongator complex (Elp1-Elp6), which disable mcm5 side chain formation, or removal of components of the thiolation pathway (Ncs2/Ncs6, Urm1, Uba4) are individually tolerated, the combination of both modification defects has been reported to have lethal effects on Saccharomyces cerevisiae. Contrary to such absolute requirement of mcm5s2U for viability, we demonstrate here that in the S. cerevisiae S288C-derived background, both pathways can be simultaneously inactivated, resulting in combined loss of tRNA anticodon modifications (mcm5U and s2U) without a lethal effect. However, an elp3 disruption strain displays synthetic sick interaction and synergistic temperature sensitivity when combined with either uba4 or urm1 mutations, suggesting major translational defects in the absence of mcm5s2U modifications. Consistent with this notion, we find cellular protein levels drastically decreased in an elp3uba4 double mutant and show that this effect as well as growth phenotypes can be partially rescued by excess of tRNALysUUU. These results may indicate a global translational or protein homeostasis defect in cells simultaneously lacking mcm5 and s2 wobble uridine modification that could account for growth impairment and mainly originates from tRNALysUUU hypomodification and malfunction.

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Objetivou-se neste trabalho avaliar a seletividade de herbicidas aplicados nas gramas Santo Agostinho (Stenotaphrum secundatum) e Esmeralda (Zoysia japonica) em condições de campo. O delineamento experimental utilizado foi o de blocos casualizados, com quatro repetições. As gramas foram cortadas a 3 cm de altura e, em seguida, foram feitas as aplicações dos herbicidas. Os tratamentos utilizados foram: testemunha sem aplicação, fluazifop-p-butil (125 g ha-1), sethoxydim+óleo mineral (276 g ha-1 + 0,5% v v-1 de Assist), bispyribac-sodium (25 g ha-1), chlorimuron-ethyl (15 g ha-1), ethoxysulfuron (150 g ha-1), halosulfuron (112,5 g ha-1), iodosulfuron-methyl (10 g ha-1), metsulfuron-methyl (2,4 g ha-1), nicosulfuron (125 g ha-1), pyrithiobac-sodium (140 g ha-1), trifloxysulfuron-sodium (22,5 g ha-1), 2,4-D (720 g ha-1), quinclorac (375 g ha-1), atrazina (1.250 g ha-1), bentazon (600 g ha-1), linuron (1.350 g ha-1), fomesafen (187,5 g ha-1), lactofen (120 g ha-1), oxadiazon (600 g ha-1) e oxyfluorfen (720 g ha-1). Os herbicidas que apresentaram potencial de seletividade para o gramado de S. secundatum foram: os inibidores da ALS chlorimuron-ethyl, ethoxysulfuron, halosulfuron, iodosulfuron-methyl e metsulfuron-methyl, o mimetizador de auxina 2,4-D, os inibidores do fotossistema II atrazina e bentazon, bem como os inibidores da Protox fomesafen, lactofen e o oxadiazon. Para o gramado de Z. japonica, os herbicidas que apresentaram potencial de seletividade foram: os inibidores da ALS chlorimuron-ethyl, ethoxysulfuron, halosulfuron, metsulfuron-methyl e nicosulfuron, os mimetizadores de auxina 2,4-D e quinclorac, os inibidores do fotossistema II atrazina e bentazon, além dos inibidores da Protox fomesafen, lactofen e o oxadiazon.

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Objetivou-se avaliar a seletividade de herbicidas aplicados na grama Batatais (Paspalum notatum) e na grama São Carlos (Axonopus compressus) em campo. O delineamento experimental utilizado foi o de blocos casualizados com quatro repetições. As gramas foram cortadas a 3 cm de altura e, em seguida, realizaram-se as aplicações dos herbicidas. Os tratamentos utilizados foram: testemunha (sem aplicação), fluazifop-p-butil (125 g ha-1), sethoxydim+óleo mineral (276 g ha-1 + 0,5% v v-1 de Assist), bispyribac-sodium (25 g ha-1), chlorimuron-ethyl (15 g ha-1), ethoxysulfuron (150 g ha-1), halosulfuron (112,5 g ha-1), iodosulfuron-methyl (10 g ha-1), metsulfuron-methyl (2,4 g ha-1), nicosulfuron (125 g ha-1), pyrithiobac-sodium (140 g ha-1), trifloxysulfuron-sodium (22,5 g ha-1), 2,4-D (720 g ha-1), quinclorac (375 g ha-1), atrazina (1.250 g ha-1), bentazon (600 g ha-1), linuron (1.350 g ha-1), fomesafen (187,5 g ha-1), lactofen (120 g ha-1), oxadiazon (600 g ha-1) e oxyfluorfen (720 g ha-1). Os herbicidas que apresentaram potencial de seletividade para o gramado de P. notatum foram o chlorimuron-ethyl, ethoxysulfuron, pyrithiobac-sodium, 2,4-D, bentazon e fomesafen; já para o gramado de A. compressus foram o chlorimuron-ethyl, ethoxysulfuron, halosulfuron, iodosulfuron-methyl, metsulfuron-methyl, pyrithiobac-sodium, 2,4-D, quinclorac, atrazina, bentazon, além do fomesafen.

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The biosynthesis of (2S)-2-methyl-2-(4'-methyl-3-pentenyl)-8-(3-methyl-2-butenyl)-2H-1-benzopyran-6-carboxylic acid (gaudichaudianic acid), the major metabolite in leaves and roots of Piper gaudichaudianum Kunth (Piperaceae), has been investigated employing [1(-13) C]-D-glucose as precursor. The labelling pattern in the isolated gaudichaudianic acid was determined by quantitative 13 C NMR spectroscopy analysis and was consistent with involvement of both mevalonic acid and 2-C-methyl-D-erythritol-4-phosphate pathways in the formation of the dimethylallyl- and geranyl-derived moieties. The results confirmed that both plastidic and cytoplasmic pathways are able to provide isopentenyl diphosphate units for prenylation of p-hydroxybenzoic acid. (c) 2007 Elsevier Ltd. All rights reserved.

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Pós-graduação em Biociências e Biotecnologia Aplicadas à Farmácia - FCFAR

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

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To obtain crystals of the Escherichia coli catabolite gene activator protein (CAP) complexed with its DNA-binding site, we have searched for crystallization conditions with 26 different DNA segments ≥28 base-pairs in length that explore a variety of nucleotide sequences, lengths, and extended 5′ or 3′ termini. In addition to utilizing uninterrupted asymmetric lac site sequences, we devised a novel approach of synthesizing half-sites that allowed us to efficiently generate symmetric DNA segments with a wide variety of extended termini and lengths in the large size range (≥28 bp) required by this protein. We report three crystal forms that are suitable for X-ray analysis, one of which (crystal form III) gives measurable diffraction amplitudes to 3 Å resolution. Additives such as calcium, n-octyl-β-d-glucopyranoside and spermine produce modest improvements in the quality of diffraction from crystal form III. Adequate stabilization of crystal form III is unexpectedly complex, requiring a greater than tenfold reduction in the salt concentration followed by addition of 2-methyl-2,4-pentanediol and then an increase in the concentration of polyethylene glycol.