RESUMEN

Carb-oxy-hydrazides are widely used in medicinal chemistry because of their medicinal properties and many drugs have been developed containing this functional group. A suitable inter-mediate to obtain potential hydrazide drug candidates is the title compound 5-hy-droxy-penta-nehydrazide, C5H12N2O2 (1). The aliphatic compound can react both via the hydroxyl and hydrazide moieties forming derivatives, which can inhibit Mycobacterium tuberculosis catalase-peroxidase (KatG) and consequently causes death of the pathogen. In this work, the hydrazide was obtained via a reaction of a lactone with hydrazine hydrate. The colourless prismatic single crystals belong to the ortho-rhom-bic space group Pca21. Regarding supra-molecular inter-actions, the compound shows classic medium to strong inter-molecular hydrogen bonds involving the hydroxyl and hydrazide groups. Besides, the three-dimensional packing also shows weak H⋯H and C⋯H contacts, as investigated by Hirshfeld surface analysis (HS) and fingerprint plots (FP).

RESUMEN

A nanosensor based on magnetic core-shell nanoparticles functionalized with rhodamine derivative, N-(3-carboxy)acryloyl rhodamine B hydrazide (RhBCARB), using (3-aminopropyl)triethoxysilane (APTES) as a linker, has been synthesized for detection of Cu(II) ions in water. The magnetic nanoparticle and the modified rhodamine were fully characterized, showing a strong orange emission sensitive to Cu(II) ions. The sensor shows a linear response from 10 to 90 µg L-1, detection limit of 3 µg L-1 and no interference of Ni(II), Co(II), Cd(II), Zn(II), Pb(II), Hg(II) and Fe(II) ions. The nanosensor performance is similar to those described in the literature, being a viable option for the determination of Cu(II) ions in natural waters. In addition, the magnetic sensor can be easily removed from the reaction medium with the aid of a magnet and its signal recovered in acidic solution, allowing its reuse in subsequent analysis.

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RESUMEN

Clinical isolates of Mycobacterium tuberculosis and Mycobacterium bovis are differentially susceptible to 2-Thiophen Hydrazide (TCH); however its mechanism of action or the reasons for that difference are unknown. We report herein that under our experimental conditions, TCH inhibits M. tuberculosis in solid but not in liquid medium, and that in spite of resembling Isoniazid and Ethionamide, it does not affect mycolic acid synthesis. To understand the mechanisms of action of TCH we isolated M. tuberculosis TCH resistant mutants which fell into two groups; one resistant to TCH and Isoniazid but not to Ethionamide or Triclosan, and the other resistant only to TCH with no, or marginal, cross resistance to Isoniazid. A S315T katG mutation conferred resistance to TCH while katG expression from a plasmid reduced M. tuberculosis MIC to this drug, suggesting a possible involvement of KatG in TCH activation. Whole genome sequencing of mutants from this second group revealed a single mutation in the alkylhydroperoxide reductase ahpC promoter locus in half of the mutants, while the remaining contained mutations in dispensable genes. This is the first report of the genetics underlying the action of TCH and of the involvement of ahpC as the sole basis for resistance to an anti-tubercular compound.

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Five new copper(II) complexes of the type [Cu(NO)(NN)(ClO4)2], in which NO=4-fluorophenoxyacetic acid hydrazide (4-FH) or 4-nitrobenzoic hydrazide (4-NH) and NN=1,10-phenanthroline (phen), 4-4'-dimethoxy-2-2'-bipyridine (dmb) or 2,2-bipyridine (bipy) were synthesized and characterized using various spectroscopic methods. The X-ray structural analysis of one representative compound indicates that the geometry around the copper ion is distorted octahedron, in which the ion is coordinated to hydrazide via the terminal nitrogen and the carbonyl oxygen, and to heterocyclic bases via their two nitrogen atoms. Two perchlorate anions occupy the apical positions, completing the coordination sphere. The cytotoxic activity of compounds was investigated in three tumor cell lines (K562, MDA-MB-231 and MCF-7). Concerning K562 cell line, the complexes with 1,10-phenanthroline exhibit high cytotoxic activity and are more active than carboplatin, free ligands and [Cu(phen)2]2+. Considering the cytotoxicity results, further investigations for the compounds [Cu(4-FH)(phen)(ClO4)2] I and [Cu(4-NH)(phen)(ClO4)2]∙H2O III were performed. Flow cytometric analysis revealed that these complexes induce apoptotic cell death in MDA-MB-231 cell line and bind to DNA with K values of 4.38×104 and 2.62×104, respectively. These compounds were also evaluated against wild type Mycobacterium tuberculosis (ATCC 27294) and exhibited antimycobacterial activity, displayed MIC values lower than those of the corresponding free ligands.

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Kinetic and mechanistic aspects of the photochemical and microbiological degradation of the herbicide Maleic Hydrazide (MH) have been studied. Riboflavin (Rf, vitamin B2) was employed as a main photosensitizer whereas Humic Acid (HA) was included as a second sensitizer in order to more closely simulate natural environmental conditions. MH quenches excited singlet and triplet states of Rf, with rate constants close to the diffusion limit. The herbicide and dissolved molecular oxygen competitively quench triplet excited Rf. As a consequence the reactive oxygen species (ROS), superoxide radical anion (O2(-·)), hydrogen peroxide (H2O2) and singlet molecular oxygen (O2((1)Δg)) are produced by electron- and energy-transfer processes, respectively, as demonstrated by auxiliary experiments employing selective auxiliary quenchers and the exclusive O2((1)Δg) generator Rose Bengal (RB). As a global result, the photodegradation of Rf is retarded, whereas MH is degraded by the generated ROS. The bacteria Pseudomonas aeruginosa (Ps) and Bacillus subtilis (Bs), recognized as contaminants surface-water and soil and microbial antagonists of phytopathogenic, were used in the microbiological experiments. Results of the individual incubation of both bacteria in in the presence of MH indicate a stimulation on the Ps growth, implying the biodegradation of the herbicide, whereas MH only exerted a bacteriostatic effect on Bs.

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The aim of this study was to investigate the response of cultivation cycle, length, width and area leaf, to the growth retardant Daminozide, sprayed on the Chrysanthemum (Dendranthema grandiflora Tzvelev.) ‘Snowdon’ cultivated in pot. The study consisted of two experiments with five repetitions. The experiments were bifactorial 4 x 2, with four concentrations of Daminozide (0, 2.000, 4.000 and 6.000 mg.L-1) and two frequencies of application (weekly and bi-weekly) of product. Cultivation cycle, leaf length, width and area were determined. The ‘Snowdon’ was able to produce pots commercially acceptable, with increase in the cultivation cycle and decrease of the leaf size.

O objetivo do trabalho foi avaliar a resposta quanto ao ciclo e comprimento, largura e área da folha, ao redutor de crescimento Daminozide, pulverizado na cultivar de crisântemo (Dendranthema grandiflora Tzvelev.) de corte Snowdon, conduzida em vaso. O estudo foi composto por dois ensaios com cinco repetições, no delineamento experimental inteiramente casualizado bifatorial 4 x 2, sendo formado por quatro doses de Daminozide (0, 2000, 4000 e 6000 mg.L-1) e duas freqüências de aplicações (semanal e bissemanal). Os resultados mostraram que a cultivar Snowdon pode ser conduzida em vaso, porém, com aumento de ciclo e redução de até 28% na área da folha.

RESUMEN

The aim of this study was to investigate the response of cultivation cycle, length, width and area leaf, to the growth retardant Daminozide, sprayed on the Chrysanthemum (Dendranthema grandiflora Tzvelev.) ‘Snowdon cultivated in pot. The study consisted of two experiments with five repetitions. The experiments were bifactorial 4 x 2, with four concentrations of Daminozide (0, 2.000, 4.000 and 6.000 mg.L-1) and two frequencies of application (weekly and bi-weekly) of product. Cultivation cycle, leaf length, width and area were determined. The ‘Snowdon was able to produce pots commercially acceptable, with increase in the cultivation cycle and decrease of the leaf size.

O objetivo do trabalho foi avaliar a resposta quanto ao ciclo e comprimento, largura e área da folha, ao redutor de crescimento Daminozide, pulverizado na cultivar de crisântemo (Dendranthema grandiflora Tzvelev.) de corte Snowdon, conduzida em vaso. O estudo foi composto por dois ensaios com cinco repetições, no delineamento experimental inteiramente casualizado bifatorial 4 x 2, sendo formado por quatro doses de Daminozide (0, 2000, 4000 e 6000 mg.L-1) e duas freqüências de aplicações (semanal e bissemanal). Os resultados mostraram que a cultivar Snowdon pode ser conduzida em vaso, porém, com aumento de ciclo e redução de até 28% na área da folha.

RESUMEN

The aim of this study was to investigate the response of potted chrysanthemum cv. Snowdon, to the growth retardant Daminozide, in terms of fenometric parameters. The study consisted of two experiments with five repetitions. The experiments were bifactorial 4 x 2, with four concentrations of Daminozide (0, 2,000, 4,000 and 6,000 mg.L-1) and two times of application (weekly and bi-weekly) of the product. Plant height, number of nodes, length of internodes, diameter of stems and inflorescences, length and diameter of floral peduncle were determinated. All concentrations and times of applications were able to reduce plant height, length of internodes, flower diameter and floral peduncle length. However, the diameter of the stem and floral peduncle were increased. The weekly application of 4,000 mg.L-1 Daminozide produced plants with the best quality within the commercial standards.

O trabalho teve como objetivo avaliar a resposta de crisântemo através da análise de parâmetros fenométricos, ao redutor de crescimento Daminozide, pulverizado na cultivar de crisântemo de corte "Snowdon", cultivada em vaso. O estudo foi formado por dois ensaios com cinco repetições, usando delineamento experimental inteiramente casualizado em esquema fatorial 4 x 2, sendo formado por quatro doses de Daminozide (0, 2.000, 4.000 e 6.000 mg.L-1) e duas freqüências de aplicações (semanal e bissemanal). Os resultados evidenciaram que as diferentes doses e freqüências de aplicações reduziram a altura da planta, o número de nós, o comprimento de entrenós, o diâmetro da inflorescência e o comprimento do pedúnculo floral. Entretanto, constatou-se aumento dos diâmetros da haste e do pedúnculo floral. Na dose 4.000 mg.L-1 aplicada semanalmente, produziram-se os vasos de melhor qualidade, com altura da planta nos padrões recomendados para comercialização.

RESUMEN

The aim of this study was to investigate the response of potted chrysanthemum cv. Snowdon, to the growth retardant Daminozide, in terms of fenometric parameters. The study consisted of two experiments with five repetitions. The experiments were bifactorial 4 x 2, with four concentrations of Daminozide (0, 2,000, 4,000 and 6,000 mg.L-1) and two times of application (weekly and bi-weekly) of the product. Plant height, number of nodes, length of internodes, diameter of stems and inflorescences, length and diameter of floral peduncle were determinated. All concentrations and times of applications were able to reduce plant height, length of internodes, flower diameter and floral peduncle length. However, the diameter of the stem and floral peduncle were increased. The weekly application of 4,000 mg.L-1 Daminozide produced plants with the best quality within the commercial standards.

O trabalho teve como objetivo avaliar a resposta de crisântemo através da análise de parâmetros fenométricos, ao redutor de crescimento Daminozide, pulverizado na cultivar de crisântemo de corte "Snowdon", cultivada em vaso. O estudo foi formado por dois ensaios com cinco repetições, usando delineamento experimental inteiramente casualizado em esquema fatorial 4 x 2, sendo formado por quatro doses de Daminozide (0, 2.000, 4.000 e 6.000 mg.L-1) e duas freqüências de aplicações (semanal e bissemanal). Os resultados evidenciaram que as diferentes doses e freqüências de aplicações reduziram a altura da planta, o número de nós, o comprimento de entrenós, o diâmetro da inflorescência e o comprimento do pedúnculo floral. Entretanto, constatou-se aumento dos diâmetros da haste e do pedúnculo floral. Na dose 4.000 mg.L-1 aplicada semanalmente, produziram-se os vasos de melhor qualidade, com altura da planta nos padrões recomendados para comercialização.

RESUMEN

One of the major limiting factor for increasing flooded rice yield potential is the interference exerted by red rice, a weedy grass. Botanically, both belong to the same species (Oryza sativa L.), which limits the utilization of selective herbicides for the control. With the objetive of investigating the effects of non-selective herbicides applied at the maturity phase of flooded rice, on agronomic characteristics of the crop, two field experiments and also laboratory evaluations were conducted during the growing seasons of 1997/98 and 1998/99. Treatments compared the herbicides glyphosate, glufosinate, and paraquat, applied at two rates and at two times, the growth regulator maleic hydrazide, applied at two times, and one check without applications of chemicals. The rice cultivar tested was IRGA-416, an early maturity variety. The management practices used were those recommended for the crop, which grew in the presence of a red rice infestation. Cultivated rice characteristics evaluated were grain yield and its components, milling yield and harvest anticipation. The non-selective herbicides glyphosate, glufosinate, and paraquat, when applied at physiological maturity stage of the cultivated rice, in general do not affect negatively the agronomic characteristics of the crop and present effects equivalent to those of the growth regulator maleic hydrazide. Differences in rates and in application times generally do not differ in relation to their actions. Desiccation action of the herbicides hastens rice grain moisture reduction and allow harvest anticipation. After the stage when flooded rice grains reach a moisture level of 34%, the maleic hydrazide growth regulator does not affect negatively crop characteristics.

Um dos principais fatores limitantes da exploração do potencial máximo de rendimento do arroz irrigado é a interferência exercida pelo arroz vermelho, uma gramínea daninha. Botanicamente, ambos pertencem a mesma espécie (Oryza sativa L.), o que limita a utilização de herbicidas seletivos para seu controle. Com o objetivo de investigar os efeitos de herbicidas não seletivos, aplicados na fase de maturação do arroz cultivado, sobre características agronômicas da cultura, conduziu-se dois experimentos a campo nas estações de crescimento de 1997/98 e 1998/99, e avaliações em laboratório. Os tratamentos compararam os herbicidas glyphosate, glufosinate e paraquat, aplicados em duas doses e duas épocas, além do regulador de crescimento hidrazida maléica, aplicada também em duas épocas, e testemunha não tratada. Como cultivar de arroz foi utilizada a IRGA-416, de ciclo precoce. As demais práticas de manejo foram aquelas preconizadas para a cultura, a qual desenvolveu-se na presença de arroz vermelho. Avaliaram-se as características do arroz cultivado, rendimento de grãos e seus componentes, rendimento de engenho e antecipação da colheita. Os herbicidas não seletivos glyphosate, glufosinate e paraquat, quando aplicados na fase de maturação fisiológica do arroz cultivado, em geral não afetam negativamente as características agronômicas da cultura e apresentam efeitos equivalentes aos do regulador de crescimento hidrazida maléica. Variações de doses e épocas de aplicação geralmente não se diferenciam quanto à ação. A ação dessecante dos herbicidas apressa a redução da umidade dos grãos de arroz e permite antecipar a colheita. A partir do estádio em que os grãos de arroz cultivado atingem teor de umidade de 34%, o regulador de crescimento hidrazida maléica não afeta negativamente as características da cultura.

RESUMEN

One of the major limiting factor for increasing flooded rice yield potential is the interference exerted by red rice, a weedy grass. Botanically, both belong to the same species (Oryza sativa L.), which limits the utilization of selective herbicides for the control. With the objetive of investigating the effects of non-selective herbicides applied at the maturity phase of flooded rice, on agronomic characteristics of the crop, two field experiments and also laboratory evaluations were conducted during the growing seasons of 1997/98 and 1998/99. Treatments compared the herbicides glyphosate, glufosinate, and paraquat, applied at two rates and at two times, the growth regulator maleic hydrazide, applied at two times, and one check without applications of chemicals. The rice cultivar tested was IRGA-416, an early maturity variety. The management practices used were those recommended for the crop, which grew in the presence of a red rice infestation. Cultivated rice characteristics evaluated were grain yield and its components, milling yield and harvest anticipation. The non-selective herbicides glyphosate, glufosinate, and paraquat, when applied at physiological maturity stage of the cultivated rice, in general do not affect negatively the agronomic characteristics of the crop and present effects equivalent to those of the growth regulator maleic hydrazide. Differences in rates and in application times generally do not differ in relation to their actions. Desiccation action of the herbicides hastens rice grain moisture reduction and allow harvest anticipation. After the stage when flooded rice grains reach a moisture level of 34%, the maleic hydrazide growth regulator does not affect negatively crop characteristics.

Um dos principais fatores limitantes da exploração do potencial máximo de rendimento do arroz irrigado é a interferência exercida pelo arroz vermelho, uma gramínea daninha. Botanicamente, ambos pertencem a mesma espécie (Oryza sativa L.), o que limita a utilização de herbicidas seletivos para seu controle. Com o objetivo de investigar os efeitos de herbicidas não seletivos, aplicados na fase de maturação do arroz cultivado, sobre características agronômicas da cultura, conduziu-se dois experimentos a campo nas estações de crescimento de 1997/98 e 1998/99, e avaliações em laboratório. Os tratamentos compararam os herbicidas glyphosate, glufosinate e paraquat, aplicados em duas doses e duas épocas, além do regulador de crescimento hidrazida maléica, aplicada também em duas épocas, e testemunha não tratada. Como cultivar de arroz foi utilizada a IRGA-416, de ciclo precoce. As demais práticas de manejo foram aquelas preconizadas para a cultura, a qual desenvolveu-se na presença de arroz vermelho. Avaliaram-se as características do arroz cultivado, rendimento de grãos e seus componentes, rendimento de engenho e antecipação da colheita. Os herbicidas não seletivos glyphosate, glufosinate e paraquat, quando aplicados na fase de maturação fisiológica do arroz cultivado, em geral não afetam negativamente as características agronômicas da cultura e apresentam efeitos equivalentes aos do regulador de crescimento hidrazida maléica. Variações de doses e épocas de aplicação geralmente não se diferenciam quanto à ação. A ação dessecante dos herbicidas apressa a redução da umidade dos grãos de arroz e permite antecipar a colheita. A partir do estádio em que os grãos de arroz cultivado atingem teor de umidade de 34%, o regulador de crescimento hidrazida maléica não afeta negativamente as características da cultura.