Synthesis, Antifungal and Antitumor Activity of Novel (Z)-5-Hetarylmethylidene-1,3-thiazol-4-ones and (Z)-5-Ethylidene-1,3-thiazol-4-ones

New hetaryl- and alkylidenerhodanine derivatives 3a-d, 3e, and 4a-d were prepared from heterocyclic aldehydes 1a-d or acetaldehyde 1e. The treatment of several rhodanine derivatives 3a-d and 3e with piperidine or morpholine in THF under reflux, afforded (Z)-5-(hetarylmethylidene)-2-(piperidin-1-yl) thiazol-4(5H)-ones and 2-morpholinothiazol-4(5H)-ones 5a-d, 6a-d, and (Z)-5-ethylidene-2-morpholinothiazol-4(5H)-one (5e), respectively, in good yields. Structures of all compounds were determined by IR, 1D and 2D NMR and mass spectrometry. Several of these compounds were screened by the U.S. National Cancer Institute (NCI) to assess their antitumor activity against 60 different human tumor cell lines. Compound 3c showed high activity against HOP-92 (Non-Small Cell Lung Cancer), which was the most sensitive cell line, with GI(50) = 0.62 mu M and LC50 > 100 mu M from the in vitro assays. In vitro antifungal activity of these compounds was also determined against 10 fungal strains. Compound 3e showed activity against all fungal strains tested, but showed high activity against Saccharomyces cerevisiae (MIC 3.9 mu g/mL).

International Activity 2008

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International Law Observatory: International Activity

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Administrative authorization for the demolition of urban rental units pursuant to the law of 1964: a spanish example of problematic over-activity in the application of transitional laws

Transitional provisions are defined as the set of regulations that rule juridical relationships on the occasion of a legislative change. Out of this context of law succession, their indiscriminate application can lead to serious inconsistencies. The analysis of a Spanish private law example is offered to illustrate this fact. It concerns the administrative authorization for the demolition of rented buildings in the cities. A regulation repealed more than fifteen years ago and however widespread utilised on ancient constructions that, after recent urban development, have acquired great economic value; something that in the end explains the current importance of such provisions. What is happening in Spain: denaturalization of the original  figure due to a mixture of formalist interpretations and speculative market interests, is presented here to call the attention on the necessary limitation of transitional provisions’ effects.

Senescence-associated β-galactosidase activity in the in vitro ovarian stromal fibroblasts

Introduction: A growing biological research field is the cellular senescence, a mechanism that has been associated, under certain circumstances, with malignant transformation. Given the high incidence of ovarian cancer and its main origin from the ovarian surface epithelium, as well as the possibility that an epithelial-mesenchymal transition occurs, we evaluated both the in vitro growth of stromal fibroblasts from the ovarian cortex and their β-galactosidase activity at pH 6, enzyme whose expression is considered as a marker of replicative senescence. Methods: 48 samples of ovarian cortical fibroblasts from donors without a history of cancer were serially cultured until the end of their replicative life. β-galactosidase activity at pH 6 was quantified in each passage by the chemiluminiscent method. As control, we used ovarian epithelial cell cultures from the same donors. The enzyme activity was also evaluated in fibroblasts previously induced to senescence by exposure to hydrogen peroxide. Results: The analysis of the enzyme activity and the replicative capacity taken together showed that the fibroblast cultures reached the senescent state at passages 4-5, as what happened with the control epithelial cells. Fibroblasts induced to senescence showed high variability in the values of enzymatic activity. Conclusions: The similarity between both types of cells in reaching the senescent state deserves to be taken into account in relation to the epithelialmesenchymal transition that has been proposed to explain their behavior in the genesis of cancer arising from ovarian surface epithelium. Low β-galactosidase activity values at pH 6 would suggest possible inactivation of the response pathways to oxidative stress.

Behavioral changes, used and benefits of a community program for the promotion in physical activity

Objective: To determine the change of behavior in physical activity and the characteristics associated with the use and benefits of Local Physical Activity Center (CLAF) in the population of the town of Santa Fe de Bogota. Materials and methods: We conducted a longitudinal study before and after, which was assessed at admission and 3 months in the intervention program CLAF physical activity, behavior change compared to the physical activity of users. Inclusion criteria: were being active user of CLAF, aged between 15 and 65 years and voluntarily express their participation in the study. Exclusion criteria: Fill incomplete measurement instruments used. The sampling frame of CLAF users, we selected n=55 subjects. To gather information, a questionnaire, which contained the behavioral stages of change, also conducted a survey which determined semistructured features about the benefits and use of CLAF. Results: The total study participants was n = 55, mean age was 40.4 ± 15.3 years, with a minimum 15 and maximum of 64 years, 83.6% were women. 78.2% do not know the purpose of the Local Centre for Physical Activity. The outreach strategy that most came to the group was 58.2 with a verbal type. The time for links to CLAF more frequently in the group evaluated was 1 to 6 months 36.4. The motivation to regularly attend the CLAF in the majority was to improve the physical and / or a 74.5% mental. 89.1% would be willing to recommend to others the use of CLAF. A 81.8% of the population physical activity performed by more than 150 min / wk at moderate intensity; Post CLAF intervention in the subjects showed positive changes in the level of physical activity (p<0.001, Test de Wilcoxon) and behavioral state (p<0.001, Test de Wilcoxon).

Pedometer: intervention strategy and physical activity promotion

World Health Organization (WHO) has prioritized physical activity (PA) as one of the mostrelevant strategies leading the decreasing prevalence of noncommunicable chronic diseases. Pedometer has emerged as one of the valid intervention programs, reliable and useful to assess,measure and promote the physical activity practice, through counts the number of steps perday. One of the aims is to establish the goals based on steps per day made by a person and thepositive feedback, which can generate behavior changes and adoption of healthy habits, from a regular physical activity practice perspective. This review attends to enhance the current state ofpedometer program, as an intervention one, in all kind of population; its health impact and theapplication methodologies, using the pedometer as a steps quantifier device, with feasible access,use and management. Additionally, the review will be useful as a framework to design futureresearch projects, aim to develop, adapt and apply evidence based pedometer protocols, insideclinical, academic and community context.

Reflections about physiotherapist professional performance in the field of physical activity

The physiotherapist professional activities, in the beginning were focused only in the clinical field, nowadays it has many different action fields including Physical Activity. Physical activity can be viewed from two dimensions: one biological, which is defined as any activity which requires energy expenditure involving the combined action of multiple systems; on the other side social, understood as a human activity concerning subjectivity conditions influenced by the environment where the individual and the community are developed. Given these dimensions as well as national and international benchmarks this paper’s objective is to present a series of reflections that the authors have done regarding the physiotherapist professional performance in the field of physical activity and the large possibilities derived from their practice in this field.

Caracterización de la exposición ocupacional a los gases, dióxido de azufre (so2), sulfuro de hidrógeno (h2s), y monóxido de carbono (co), y la percepción de salud de los trabajadores, en una empresa del sector hidrocarburo en Colombia

En el proceso de extracción de petróleo (crudo) deben realizarse tratamientos físicos y químicos en estaciones de recolección del hidrocarburo con el fin de garantizar su calidad antes de su entrega para el transporte y comercialización. Para la realización de esta actividad el personal operativo requerido (operadores) debe realizar diferentes actividades, tales como ronda operacional, verificación de sistemas de almacenamiento del crudo, agua residual del proceso e insumos químicos utilizados en su tratamiento y manipulación de facilidades en las estaciones de recolección, entre otras. Como resultados de las actividades rutinarias los operadores están expuestos a factores de riesgo químico asociados a gases y vapores orgánicos generados en los procesos de tratamiento del crudo. En el presente trabajo se realizaron mediciones de calidad de aire e higiene industrial en diferentes estaciones tratamiento de crudo, con el propósito de evaluar los niveles de exposición de los operadores a gases y vapores de hidrocarburos durante el proceso de tratamiento de crudo y dar respuesta a la siguiente pregunta: ¿existe relación entre la exposición ocupacional, las emisiones atmosféricas de gases (SO2, CO, H2S) y la percepción de afectación de la salud de los trabajadores que se encuentran expuestos durante la actividad laboral, en una empresa del sector de hidrocarburos? Se realizó un estudio de corte transversal, mediante la aplicación de cuestionarios sobre las condiciones de trabajo y de salud a 30 trabajadores que laboran en una estación de tratamiento de crudo de una compañía del sector de hidrocarburos. Los operadores objeto de estudio laboran en turnos rotativos, han estado vinculados con la compañía por más de dos años y tienen contrato directo, adicionalmente, se identificaron los factores de riesgos ambientales y ocupacionales para el grupo de trabajadores y se realizó una revisión de los informes de medición de higiene industrial y de calidad de aire de las estaciones donde labora el personal seleccionado con el fin de establecer si los resultados se relacionan. Los resultados obtenidos indican que el 100% de los trabajadores son de género masculino y se desempeñan en cargos de operadores, recorredores de pozos de crudo y supervisores. El 97% de los operadores tiene más de cuarenta años de edad y el 80% de los mismos ha laborado por más de 6 años en la compañía. Acerca de la percepción de los trabajadores sobre su estado de salud el 90% afirma que su salud es buena, el 97% respondió que no presenta problemas respiratorios, el 23% manifiesta que presenta trastornos dermatológicos y el 27% indican que presenta dolor de cabeza constante. De la revisión de los informes de calidad de aire disponibles se encontró que las mediciones de Dióxido de Azufre SO2, Monóxido de Carbono CO se encuentran dentro del rango definido como el de menor impacto para la salud humana. De los datos del informe se puede concluir que la calidad del aire es buena en el 100% de las áreas de influencia de las estaciones de tratamiento de crudo. Según los informes de higiene industrial el 34% de las instalaciones presenta concentraciones de Sulfuro de Hidrógeno (H2S) en el límite permisible para exposiciones crónicas en un promedio ponderado de tiempo (TLV-TWA) y el límite permisible para exposiciones agudas en un límite de exposición a corto plazo (TLV-STEL). Solo el 37% de los trabajadores objeto de este estudio percibe el riesgo por la exposición a factores de riesgo químicos y son claramente consientes que se encuentran expuestos a estos riesgos por la manipulación de productos químicos y exposición a sustancias químicas producto de sus actividades rutinarias, el 73% no percibe el riesgo de exposición por su actividad laboral. Se recomienda que la compañía fortalezca su esquema de vigilancia para generar alternativas que eleven los niveles de consciencia del riesgo del trabajador. Los factores de riesgo ambiental y ocupacional, de los gases y vapores generados se deben al proceso de tratamiento de crudo, están mutuamente relacionados dado que al generarse una emisión y/o escape no controlado como consecuencia se tiene una afectación directa al medio ambiente y a los trabajadores.

Political intervention in economic activity

This paper proposes a political economy explanation of bailouts to declining industries. A model of probabilistic voting is developed, in which two candidates compete for the vote of two groups of the society through tactical redistribution. We allow politicians to have core support groups they understand better, this implies politicians are more or less effective to deliver favors to some groups. This setting is suited to reproduce pork barrels or machine politics and patronage. We use this model to illustrate the case of an economy with both an efficient industry and a declining one, in which workers elect their government. We present the conditions under which the political process ends up with the lagged-behind industry being allowed to survive.