Eight new 5-arylidene-3-benzyl-thiazolidine-2,4-diones with halide groups on their benzyl rings were synthesized and assayed in vivo to investigate their anti-inflammatory activities. These compounds showed considerable biological efficacy when compared to rosiglitazone, a potent and well-known agonist of PPARgamma, which was used as a reference drug. This suggests that the substituted 5-arylidene and 3-benzylidene groups play important roles in the anti-inflammatory properties of this class of compounds. Docking studies with these compounds indicated that they exhibit specific interactions with key residues located in the site of the PPARgamma structure, which corroborates the hypothesis that these molecules are potential ligands of PPARgamma. In addition, competition binding assays showed that four of these compounds bound directly to the ligand-binding domain of PPARgamma, with reduced affinity when compared to rosiglitazone. An important trend was observed between the docking scores and the anti-inflammatory activities of this set of molecules. The analysis of the docking results, which takes into account the hydrophilic and hydrophobic interactions between the ligands and the target, explained why the 3-(2-bromo-benzyl)-5-(4-methanesulfonyl-benzylidene)-thiazolidine-2,4-dione compound had the best activity and the best docking score. Almost all of the stronger hydrophilic interactions occurred between the substituted 5-arylidene group of this compound and the residues of the binding site.

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In this work, the acridine nucleus was used as a lead-compound for structural modification by adding different substituted thiosemicarbazide moieties. Eight new (Z)-2-(acridin-9-ylmethylene)-N-phenylhydrazinecarbothioamide derivatives (3a–h) were synthesized, their antiproliferative activities were evaluated, and DNA binding properties were performed with calf thymus DNA (ctDNA) by electronic absorption and fluorescence spectroscopies. Both hyperchromic and hypochromic effects, as well as red or blue shifts were demonstrated by addition of ctDNA to the derivatives. The calculated binding constants ranged from 1.74 × 104 to 1.0 × 106 M−1 and quenching constants from −0.2 × 104 to 2.18 × 104 M−1 indicating high affinity to ctDNA base pairs. The most efficient compound in binding to ctDNA in vitro was (Z)-2-(acridin-9-ylmethylene)-N-(4-chlorophenyl) hydrazinecarbothioamide (3f), while the most active compound in antiproliferative assay was (Z)-2-(acridin-9-ylmethylene)-N-phenylhydrazinecarbothioamide (3a). There was no correlation between DNA-binding and in vitro antiproliferative activity, but the results suggest that DNA binding can be involved in the biological activity mechanism. This study may guide the choice of the size and shape of the intercalating part of the ligand and the strategic selection of substituents that increase DNA-binding or antiproliferative properties.

BackgroundThe use of interdisciplinary approaches such as the proposed report provides a broad understanding of the relationship between people and the environment, revealing reliable aspects not previously considered in the study of this relationship. This study compiled evidence on the environmental degradation of an urbanized river over the past few decades, providing a diagnosis of the consequences of this process for the river, its ichthyofauna, and the local human population.MethodsThe study was focused on the Beira Rio community on the Capibaribe River in the municipality of São Lourenço da Mata, Pernambuco, Brazil. Data were collected using geoprocessing and ethnobiological approaches, as well as environmental parameters. This research was conducted with the most experienced long-term residents in the local community, through interviews and participatory methodologies to recovering information about the river environment, its ichthyofauna and its environmental services for the last decades.ResultsAccording to the GIS analysis, the study area was subject to an accelerated process of urbanization, with the total urban area increasing from 73 565, 98 m2 in 1974 to 383 363, 6 m2 in 2005. The informants perceived the urban growth, especially in the late twentieth century, being this period recognized as the phase of greatest negative changes in the river environment. The perceived decline of fish stocks was indicated by the community as one of the effects of river degradation. According to the interviews, the deterioration of the river affected the ecosystem services and the relationship of the adjacent human community with this ecosystem. The environmental data indicated that the river is suffering eutrophization and has fecal coliform concentrations 160 times higher than the maximum level permitted by Brazilian legislation.ConclusionsThe interdisciplinary approach used in this research allowed the understanding of the degradation process of an urban river and some negative effects through the integration of environmental data, GIS and the local knowledge, revealing the complementarity of obtained data and the effectiveness of implementation of this approach.

As rápidas mudanças espaço temporal do uso e cobertura do solo em ambiente urbano apresentam grande impacto nas relações entre os ciclos energéticos e hidrológicos sobre a superfície. Para Lombardo o clima urbano é um sistema que abrange o clima de um dado espaço terrestre e a sua urbanização é o resultado de ações antrópicas conjugadas com os aspectos geoambientais do sítio urbano. As áreas vegetadas se apresentam como importantes agentes de amenização da temperatura em ambiente urbano promovendo a redução do consumo de energia e o aumento da qualidade do ar. Deste modo o objetivo deste artigo é visualizar a disposição da temperatura da superfície para os diferentes alvos presentes no município de Recife através de imagens TM Landsat 5 e aplicar o TsHARP para identificar a influência dos diferentes materiais construtivos nos valores de temperatura da superfície. Para tal foram utilizadas oito imagens TM do satélite Landsat 5 de orbita e pontos 214/65 e 66. Todas as imagens foram préprocessadas e ortorretificadas. Para a obtenção da temperatura da superfície foi utilizada a metodologia desenvolvida por Allen e Bastiaanssen e para a reamostragem da resolução espacial da banda do termal para 30m foi utilizada a técnica TsHARP proposta por Agam. Foi observada que as áreas vegetadas conseguiram manter temperaturas mais amenas em períodos chuvosos ou secos. Em alguns casos as grandes áreas vegetadas apresentavam diferença de oito graus com relação a áreas impermeabilizadas ou construídas. Os grandes empreendimentos e estacionamentos que apresentavam boa arborização demonstraram temperaturas mais baixas do que os que não possuíam. Palavras-chave: Landsat, TsHARP, Ilhas de Amenidade, Distribuição da vegetação. Use and Soil Cover and its Efects on Distribution of the Surface Temperature on Urban Area A B S T R A C T Rapid changes timeline use and land cover in urban environment have great impact on relations between the energy and hydrological cycles on the surface. Lombardo for the urban climate is a system that covers the climate of a given land space and its urbanization is the result of human actions, combined with the geo-environmental aspects of the urban site. The vegetated areas present them selves as important agents softening temperature in the urban environment by promoting the reduction of energy consumption and increase air quality. Thus the aim of this article is to visualize the layout of the surface temperature for different targets present in the city of Recife by Landsat 5TM images and apply TsHARP to identify the influence of different building materials in the values of surface temperature. To this we used eight images of Landsat 5 TM orbital points and 214/65 and 66. All images were pre-processed and orthorectified. To obtain the surface temperature was used the methodology developed by Allen and Bastiaanssen an dresampling of the spatial resolution of the thermal band to 30m technique was used TsHARP proposed by Agam. It was observed that the vegetated areas were able to maintain lower temperatures ...