Synthesis of benzylpiperazine derivatives containing the pyrazine moiety with potential activity against M. tuberculosis/Síntese de derivados da benzilpiperazina contendo a fracção pirazina com potencial actividade contra a M. tuberculosis

A tuberculose (TB) ainda é um problema de saúde pública global, apesar dos esforços e recentes avanços na medicina e farmacologia. A Organização Mundial da Saúde estima que em 2018, 1,5 milhões de pessoas morreram em todo o mundo devido à tuberculose. Nesse contexto, é urgente a busca por novas moléculas que possam oferecer mais eficácia, menor tempo de tratamento, com menores efeitos adversos conta TB. O presente trabalho descreve a síntese de oito novas benzilpiperazinas contendo o núcleo pirazina, com potencial atividade antituberculose. As moléculas foram planejadas de maneira racional, utilizando-se a técnica de hibridação molecular, a partir do fármaco pirazinamida e do núcleo benzilpiperazina. As substâncias propostas foram obtidas a partir de um processo sintético simples e reprodutivo, em rendimentos baixos

Synthesis and Biological Aspects of Mycolic Acids: An Important Target Against Mycobacterium tuberculosis

Mycolic acids are an important class of compounds, basically found in the cell walls of a group of bacteria known as mycolata taxon, exemplified by the most famous bacteria of this group, the Mycobacterium tuberculosis (M. tb.), the agent responsible for the disease known as tuberculosis (TB). Mycolic acids are important for the survival of M. tb. For example, they are able to help fight against hydrophobic drugs and dehydration, and also allow this bacterium to be more effective in the host's immune system by growing inside macrophages. Due to the importance of the mycolic acids for maintenance of the integrity of the mycobacterial cell wall, these compounds become attractive cellular targets for the development of novel drugs against TB. In this context, the aim of this article is to highlight the importance of mycolic acids in drug discovery

Mitochondrial physiology

As the knowledge base and importance of mitochondrial physiology to evolution, health and disease expands, the necessity for harmonizing the terminology concerning mitochondrial respiratory states and rates has become increasingly apparent. The chemiosmotic theory establishes the mechanism of energy transformation and coupling in oxidative phosphorylation. The unifying concept of the protonmotive force provides the framework for developing a consistent theoretical foundation of mitochondrial physiology and bioenergetics. We follow the latest SI guidelines and those of the International Union of Pure and Applied Chemistry (IUPAC) on terminology in physical chemistry, extended by considerations of open systems and thermodynamics of irreversible processes. The concept-driven constructive terminology incorporates the meaning of each quantity and aligns concepts and symbols with the nomenclature of classical bioenergetics. We endeavour to provide a balanced view of mitochondrial respiratory control and a critical discussion on reporting data of mitochondrial respiration in terms of metabolic flows and fluxes. Uniform standards for evaluation of respiratory states and rates will ultimately contribute to reproducibility between laboratories and thus support the development of data repositories of mitochondrial respiratory function in species, tissues, and cells. Clarity of concept and consistency of nomenclature facilitate effective transdisciplinary communication, education, and ultimately further discovery

Mitochondrial physiology

As the knowledge base and importance of mitochondrial physiology to evolution, health and disease expands, the necessity for harmonizing the terminology concerning mitochondrial respiratory states and rates has become increasingly apparent. The chemiosmotic theory establishes the mechanism of energy transformation and coupling in oxidative phosphorylation. The unifying concept of the protonmotive force provides the framework for developing a consistent theoretical foundation of mitochondrial physiology and bioenergetics. We follow the latest SI guidelines and those of the International Union of Pure and Applied Chemistry (IUPAC) on terminology in physical chemistry, extended by considerations of open systems and thermodynamics of irreversible processes. The concept-driven constructive terminology incorporates the meaning of each quantity and aligns concepts and symbols with the nomenclature of classical bioenergetics. We endeavour to provide a balanced view of mitochondrial respiratory control and a critical discussion on reporting data of mitochondrial respiration in terms of metabolic flows and fluxes. Uniform standards for evaluation of respiratory states and rates will ultimately contribute to reproducibility between laboratories and thus support the development of data repositories of mitochondrial respiratory function in species, tissues, and cells. Clarity of concept and consistency of nomenclature facilitate effective transdisciplinary communication, education, and ultimately further discovery

Prevalence, associated factors and outcomes of pressure injuries in adult intensive care unit patients: the DecubICUs study

Funder: European Society of Intensive Care Medicine; doi: http://dx.doi.org/10.13039/501100013347Funder: Flemish Society for Critical Care NursesAbstract: Purpose: Intensive care unit (ICU) patients are particularly susceptible to developing pressure injuries. Epidemiologic data is however unavailable. We aimed to provide an international picture of the extent of pressure injuries and factors associated with ICU-acquired pressure injuries in adult ICU patients. Methods: International 1-day point-prevalence study; follow-up for outcome assessment until hospital discharge (maximum 12 weeks). Factors associated with ICU-acquired pressure injury and hospital mortality were assessed by generalised linear mixed-effects regression analysis. Results: Data from 13,254 patients in 1117 ICUs (90 countries) revealed 6747 pressure injuries; 3997 (59.2%) were ICU-acquired. Overall prevalence was 26.6% (95% confidence interval [CI] 25.9–27.3). ICU-acquired prevalence was 16.2% (95% CI 15.6–16.8). Sacrum (37%) and heels (19.5%) were most affected. Factors independently associated with ICU-acquired pressure injuries were older age, male sex, being underweight, emergency surgery, higher Simplified Acute Physiology Score II, Braden score 3 days, comorbidities (chronic obstructive pulmonary disease, immunodeficiency), organ support (renal replacement, mechanical ventilation on ICU admission), and being in a low or lower-middle income-economy. Gradually increasing associations with mortality were identified for increasing severity of pressure injury: stage I (odds ratio [OR] 1.5; 95% CI 1.2–1.8), stage II (OR 1.6; 95% CI 1.4–1.9), and stage III or worse (OR 2.8; 95% CI 2.3–3.3). Conclusion: Pressure injuries are common in adult ICU patients. ICU-acquired pressure injuries are associated with mainly intrinsic factors and mortality. Optimal care standards, increased awareness, appropriate resource allocation, and further research into optimal prevention are pivotal to tackle this important patient safety threat

Correction to: Prevalence, associated factors and outcomes of pressure injuries in adult intensive care unit patients: the DecubICUs study

The original version of this article unfortunately contained a mistake

Prevalence, associated factors and outcomes of pressure injuries in adult intensive care unit patients: the DecubICUs study

Funder: European Society of Intensive Care Medicine; doi: http://dx.doi.org/10.13039/501100013347Funder: Flemish Society for Critical Care NursesAbstract: Purpose: Intensive care unit (ICU) patients are particularly susceptible to developing pressure injuries. Epidemiologic data is however unavailable. We aimed to provide an international picture of the extent of pressure injuries and factors associated with ICU-acquired pressure injuries in adult ICU patients. Methods: International 1-day point-prevalence study; follow-up for outcome assessment until hospital discharge (maximum 12 weeks). Factors associated with ICU-acquired pressure injury and hospital mortality were assessed by generalised linear mixed-effects regression analysis. Results: Data from 13,254 patients in 1117 ICUs (90 countries) revealed 6747 pressure injuries; 3997 (59.2%) were ICU-acquired. Overall prevalence was 26.6% (95% confidence interval [CI] 25.9–27.3). ICU-acquired prevalence was 16.2% (95% CI 15.6–16.8). Sacrum (37%) and heels (19.5%) were most affected. Factors independently associated with ICU-acquired pressure injuries were older age, male sex, being underweight, emergency surgery, higher Simplified Acute Physiology Score II, Braden score 3 days, comorbidities (chronic obstructive pulmonary disease, immunodeficiency), organ support (renal replacement, mechanical ventilation on ICU admission), and being in a low or lower-middle income-economy. Gradually increasing associations with mortality were identified for increasing severity of pressure injury: stage I (odds ratio [OR] 1.5; 95% CI 1.2–1.8), stage II (OR 1.6; 95% CI 1.4–1.9), and stage III or worse (OR 2.8; 95% CI 2.3–3.3). Conclusion: Pressure injuries are common in adult ICU patients. ICU-acquired pressure injuries are associated with mainly intrinsic factors and mortality. Optimal care standards, increased awareness, appropriate resource allocation, and further research into optimal prevention are pivotal to tackle this important patient safety threat

O impacto da utilização do friso cronológico na avaliação dos alunos a Estudo do Meio Social no 1.º ciclo do ensino básico

Sendo o friso cronológico simples um recurso utilizado no processo de ensino-aprendizagem de conteúdos da História nas aulas de Estudo do Meio, foi realizada uma investigação com o objetivo de analisar o impacto da utilização deste recurso na avaliação dos alunos dos 3.º e 4.º anos de escolaridade na área disciplinar referida. Metodologicamente, a investigação segue uma abordagem quantitativa, baseada nos dados disponibilizados pelo conjunto de docentes inquiridos, quer nos questionários aplicados, quer nas grelhas relativas à avaliação dos alunos a Estudo do Meio e, em particular, em conteúdos da História e Geografia de Portugal. A análise dos dados recolhidos permite encarar com otimismo o impacto da utilização do recurso referido nas classificações dos alunos. Contudo, não foi possível comprovar uma relação direta entre esses dois fatores, dada a inexistência de dados relativos à avaliação de alunos cujos docentes não utilizam o friso cronológico. De certa forma, a investigação evidencia a importância do envolvimento dos alunos na sua construção. Contudo, os resultados indiciam a necessidade de se realizar uma abordagem sistemática e contínua do friso cronológico com os alunos em contexto de sala de aula.The impact of the use of the timeline for the evaluation of students of Social Studies of the 1st cycle of basic education Timeline is a resource used for teaching and learning History in Social Studies classes, so an investigation was carried out in order to analyze the impact of the use of this resource on the evaluation of students of the 3rd and 4th years in that subject area. Methodologically, the research follows a quantitative approach, based on data provided by the group of surveyed teachers, both in questionnaires and grids for the evaluation of students, in particular on contents of History and Geography of Portugal. The analysis of the data collected allows us to face with optimism the impact of the utilization of this resource for the evaluation of students. However, it was not possible to prove a direct relationship between these two factors, given the absence of data relating to the evaluation of students whose teachers do not use the timeline. The research highlights the importance of student involvement in its construction. However, the results indicate the need to perform a systematic and continuous approach to timeline with the students in classroom context.info:eu-repo/semantics/publishedVersio

Produtos Naturais em Fase Avançada de Testes Clínicos no Tratamento contra o Câncer

Made available in DSpace on 2017-06-01T18:43:46Z (GMT). No. of bitstreams: 2 license.txt: 1748 bytes, checksum: 8a4605be74aa9ea9d79846c1fba20a33 (MD5) 2.pdf: 2496918 bytes, checksum: ac141bcc362912e5122adbb57096a3ef (MD5) Previous issue date: 18Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil / Universidade Federal do Rio de Janeiro. Instituto de Química. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil / Universidade Federal Fluminense. Instituto de Química. Centro de Estudos Gerais. Niterói, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil / Universidade Federal do Rio de Janeiro. Instituto de Química. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil / Universidade Federal Fluminense. Instituto de Química. Centro de Estudos Gerais. Niterói, RJ, Brasil.Atualmente, os produtos naturais representam uma inestimável fonte de substâncias químicas tendo um importante papel no tratamento do câncer. Devido à importância da natureza como fonte de novos candidatos a fármacos no tratamento contra o câncer, o objetivo dessa revisão é enfocar os produtos naturais, que estão em fase avançada de testes clínicos e dentre em breve poderão ser introduzidos no mercado no combate ao câncer. Nowadays, natural products represent an outstanding source of compounds that play an important role in cancer treatment. Due to the importance of nature as a source of new cancer drugs candidates, the aim of this review is to highlight natural products, which are under clinical trials against this disease