Introducing online teaching in Humanities: A case study about the acceptance of online activities by the academic staff of classical languages

The purpose of this paper is to show the perceptions of the academic staff of classical languages (ancient Greek and Latin) concerning use of online activities during their courses. The study was carried out in three countries: Greece (three major Universities), Spain (University of Barcelona) and the United States (University of California, Berkeley) with the participation of thirty-three academic instructors. Depending on the level of use and acceptance of the ICT and following G. Moore¿s classification, we separated the participating academics in three groups: the conservatives, the mainstream and the early adopters. The fact that the smallest group is the third clearly shows the necessity for teachers¿ preparation and training before introducing innovative projects in the classroom. Since the starting point for the application of innovation in the classroom is the teacher, policy makers should focus on helping them become conscious of changes in teaching methods and include their opinion during the design of innovative projects.

Introducing online teaching in Humanities: A case study about the acceptance of online activities by the academic staff of classical languages

The purpose of this paper is to show the perceptions of the academic staff of classical languages (ancient Greek and Latin) concerning use of online activities during their courses. The study was carried out in three countries: Greece (three major Universities), Spain (University of Barcelona) and the United States (University of California, Berkeley) with the participation of thirty-three academic instructors. Depending on the level of use and acceptance of the ICT and following G. Moore¿s classification, we separated the participating academics in three groups: the conservatives, the mainstream and the early adopters. The fact that the smallest group is the third clearly shows the necessity for teachers¿ preparation and training before introducing innovative projects in the classroom. Since the starting point for the application of innovation in the classroom is the teacher, policy makers should focus on helping them become conscious of changes in teaching methods and include their opinion during the design of innovative projects.

Enseñar a aprender a pensar en los centros educativos, incluso en las actividades de evaluación.= Teaching to learn how to think at schools, even within assessment activities

El auténtico protagonismo de los centros educativostiene que dirigirse a ayudar a pensar a sus alumnos y aenseñarlos a aprender, es decir, el docente tiene queenseñar estrategias de aprendizaje y debe promover elesfuerzo del estudiante para facilitar la construcción deesquemas y el aprendizaje permanente.El profesor debe utilizar cualquier situación deaprendizaje para enseñar dichas estrategias deaprendizaje, incluso en las situaciones de evaluación;por lo tanto, en este trabajo se sugiere que en lasevaluaciones de los alumnos y alumnas se tenga encuenta la metacognición como factor fundamental en elaprendizaje y la enseñanza

1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies

A series of 1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridines differently substituted at positions 1, 5, and 9 have been designed from the pyrano[3,2-c]quinoline derivative 1, a weak inhibitor of acetylcholinesterase (AChE) with predicted ability to bind to the AChE peripheral anionic site (PAS), at the entrance of the catalytic gorge. Fourteen novel benzonaphthyridines have been synthesized through synthetic sequences involving as the key step a multicomponent Povarov reaction between an aldehyde, an aniline and an enamine or an enamide as the activated alkene. The novel compounds have been tested against Electrophorus electricus AChE (EeAChE), human recombinant AChE (hAChE), and human serum butyrylcholinesterase (hBChE), and their brain penetration has been assessed using the PAMPA-BBB assay. Also, the mechanism of AChE inhibition of the most potent compounds has been thoroughly studied by kinetic studies, a propidium displacement assay, and molecular modelling. We have found that a seemingly small structural change such as a double O → NH bioisosteric replacement from the hit 1 to 16a results in a dramatic increase of EeAChE and hAChE inhibitory activities (>217- and >154-fold, respectively), and in a notable increase in hBChE inhibitory activity (> 11-fold), as well. An optimized binding at the PAS besides additional interactions with AChE midgorge residues seem to account for the high hAChE inhibitory potency of 16a (IC50 = 65 nM), which emerges as an interesting anti-Alzheimer lead compound with potent dual AChE and BChE inhibitory activities.

1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies

A series of 1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridines differently substituted at positions 1, 5, and 9 have been designed from the pyrano[3,2-c]quinoline derivative 1, a weak inhibitor of acetylcholinesterase (AChE) with predicted ability to bind to the AChE peripheral anionic site (PAS), at the entrance of the catalytic gorge. Fourteen novel benzonaphthyridines have been synthesized through synthetic sequences involving as the key step a multicomponent Povarov reaction between an aldehyde, an aniline and an enamine or an enamide as the activated alkene. The novel compounds have been tested against Electrophorus electricus AChE (EeAChE), human recombinant AChE (hAChE), and human serum butyrylcholinesterase (hBChE), and their brain penetration has been assessed using the PAMPA-BBB assay. Also, the mechanism of AChE inhibition of the most potent compounds has been thoroughly studied by kinetic studies, a propidium displacement assay, and molecular modelling. We have found that a seemingly small structural change such as a double O → NH bioisosteric replacement from the hit 1 to 16a results in a dramatic increase of EeAChE and hAChE inhibitory activities (>217- and >154-fold, respectively), and in a notable increase in hBChE inhibitory activity (> 11-fold), as well. An optimized binding at the PAS besides additional interactions with AChE midgorge residues seem to account for the high hAChE inhibitory potency of 16a (IC50 = 65 nM), which emerges as an interesting anti-Alzheimer lead compound with potent dual AChE and BChE inhibitory activities.

1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies

A series of 1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridines differently substituted at positions 1, 5, and 9 have been designed from the pyrano[3,2-c]quinoline derivative 1, a weak inhibitor of acetylcholinesterase (AChE) with predicted ability to bind to the AChE peripheral anionic site (PAS), at the entrance of the catalytic gorge. Fourteen novel benzonaphthyridines have been synthesized through synthetic sequences involving as the key step a multicomponent Povarov reaction between an aldehyde, an aniline and an enamine or an enamide as the activated alkene. The novel compounds have been tested against Electrophorus electricus AChE (EeAChE), human recombinant AChE (hAChE), and human serum butyrylcholinesterase (hBChE), and their brain penetration has been assessed using the PAMPA-BBB assay. Also, the mechanism of AChE inhibition of the most potent compounds has been thoroughly studied by kinetic studies, a propidium displacement assay, and molecular modelling. We have found that a seemingly small structural change such as a double O → NH bioisosteric replacement from the hit 1 to 16a results in a dramatic increase of EeAChE and hAChE inhibitory activities (>217- and >154-fold, respectively), and in a notable increase in hBChE inhibitory activity (> 11-fold), as well. An optimized binding at the PAS besides additional interactions with AChE midgorge residues seem to account for the high hAChE inhibitory potency of 16a (IC50 = 65 nM), which emerges as an interesting anti-Alzheimer lead compound with potent dual AChE and BChE inhibitory activities.

Comparação do desempenho da lipase de candida rugosa imobilizada em suporte híbrido de polissiloxano-polivinilálcool empregando diferentes metodologias

The efficiency for immobilizing microbial Candida rugosa lipase on a hybrid matrix of polysiloxane polyvinyl alcohol, by adsorption, covalent coupling and encapsulation was compared. The activities of immobilized derivatives were evaluated using p-nitrophenylpalmitate (hydrolysis) and butyric acid and butanol (esterification) as substrates. Operational stability and storage tests were also performed. Among the procedures tested, the proposed matrix was efficient for immobilizing C. rugosa lipase by adsorption and covalent coupling techniques and unsuitable for encapsulation purposes. The results reveal that better catalytic properties in both aqueous and organic media were demonstrated by the covalent coupling POS-PVA immobilized lipase, including also satisfactory half-life and good storage stability.

Natural occurrence, biological activities and synthesis of eight-, nine-, and eleven-membered ring lactones

The natural occurrence, biological activities and synthetic approaches to natural eight-, nine-, and eleven-membered lactones is reviewed. These medium ring lactones are grouped according to ring size, and their syntheses are discussed. The structures of some natural products early identified as medium-ring lactones were revised after total synthesis.

Challenges and Means for the Front End Activities of Software Development

The front end of innovation is regarded as one of the most important steps in building new software products or services, and the most significant benefits in software development can be achieved through improvements in the front end activities. Problems in the front end phase have an impact on customer dissatisfaction with delivered software, and on the effectiveness of the entire software development process. When these processes are improved, the likelihood of delivering high quality software and business success increases. This thesis highlights the challenges and problems related to the early phases of software development, and provides new methods and tools for improving performance in the front end activities of software development. The theoretical framework of this study comprises two fields of research. The first section belongs to the field of innovation management, and especially to the management of the early phases of the innovation process, i.e. the front end of innovation. The second section of the framework is closely linked to the processes of software engineering, especially to the early phases of the software development process, i.e. the practice of requirements engineering. Thus, this study extends the theoretical knowledge and discloses the differences and similarities in these two fields of research. In addition, this study opens up a new strand for academic discussion by connecting these research directions. Several qualitative business research methodologies have been utilized in the individual publications to solve the research questions. The theoretical and managerial contribution of the study can be divided into three areas: 1) processes and concepts, 2) challenges and development needs, and 3) means and methods for the front end activities of software development. First, the study discloses the difference and similarities between the concepts of the front end of innovation and requirements engineering, and proposes a new framework for managing the front end of the software innovation process, bringing business and innovation perspectives into software development. Furthermore, the study discloses managerial perceptions of the similarities and differences in the concept of the front end of innovation between the software industry and the traditional industrial sector. Second, the study highlights the challenges and development needs in the front end phase of software development, especially challenges in communication, such as linguistic problems, ineffective communication channels, a communication gap between users/customers and software developers, and participation of multiple persons in software development. Third, the study proposes new group methods for improving the front end activities of software development, especially customer need assessment, and the elicitation of software requirements.

Antioxidant and cytotoxic activities of 'açaí' (Euterpe precatoria Mart.)

Decoction of roots of the Amazonian palm açaí (Euterpe precatoria Mart.) is widely used by Brazilian and Peruvian people as an anti-inflammatory, to heal kidney and liver diseases and against snake bites. In this study, the antioxidant activity of extracts and flavonoids (quercetin, catechin, epicatechin, rutin and astilbin) isolated from roots and leaf stalks of E. precatoria was investigated using β-carotene in TLC plates and DPPH radical scavenging in a spectrophotometric bioassay. All extracts and flavonoids showed activity. Also, the cytotoxic activity of these extracts was evaluated by the brine shrimp (Artemia salina) larvicide bioassay and was lower than that of lapachol, used as control. The presence of flavonoids and sitosterol-3-O-β-D-glucopyranoside in the extracts can justify the use of the plant in traditional medicine.

In vitro antimicrobial and antioxidant activities of a crude extract and fractions from Buddleja thyrsoides Lam. Leaves

Crude extract and fractions of Buddleja thyrsoides were investigated regarding antioxidant activities by DPPH, total phenolic contents by Folin-Ciocalteau and antimicrobial activity by the broth microdilution method. Total phenolics varied from 214.07 ± 3.6 to 438.4 ± 0.3 mg g-1. Crude extract, ethyl acetate, dichloromethane and butanolic fractions exhibited a weak scavenging activity (SC50=186.04 ± 10.8, 137.70 ± 8.5, 146.89 ± 9.0 and 165.71 ± 3.2 µg mL-1, respectively). A correlation between the antioxidant activities and total phenolic contents could be shown (r=0.857, p<0.01). The lowest value of MIC was observed with butanolic fraction against Saccharomyces cerevisiae (MIC and MFC at 62.5 µg mL-1). Dichloromethane and ethyl acetate fractions were effective against Staphylococcus aureus with MIC value at 250 and 500 µg mL-1 respectively.

Influence of basic properties of Mg,Al-mixed oxides on their catalytic activity in knoevenagel condensation between benzaldehyde and phenylsulfonylacetonitrile

The catalytic performance of Mg,Al-mixed oxides (MO20, MO25 and MO33) derived from hydrotalcites was evaluated in the Knoevenagel reaction between benzaldehyde and phenylsulfonylacetonitrile at 373 and 383 K. The best results were obtained for the sample MO20 that presented the highest basic sites density and external area and the smallest crystallite sizes. The relative amount of basic sites with weak to intermediate strength also played an important role on catalytic performance. By increasing the catalyst content from 1 to 5 wt.% at 383 K, a complete conversion of the reactants is attained, producing α-phenylsulfonylcinnamonitrile with a selectivity of 100%.

Chemical composition and antibacterial activities from the essential oils of myrtaceae species planted in Brazil

The essential oils of seven Myrtaceae species were investigated for its chemical composition and antibacterial activity. The volatile oils were characterized by a high content of monoterpenoids of which 1,8-cineole (88.0, 65.0 and 77.0% for Melaleuca hypericifolia, Callistemon viminalis and Callistemon citrinus respectively), terpinen-4-ol (47.0 and 49.8% for Melaleuca thymifolia and Callistemon polandii respectively) and α-pinene (54.5% for Kunzea ericoides) were the major components. The oil from M. linariifolia was characterized by a high concentration of methyleugenol (87.2%). The oil from Melaleuca thymifolia was the most active, exhibiting high antimicrobial activity against all tested bacteria.

Preparation and characterization oF Ru-Sn/Al2O3 catalysts for the hydrogenation of fatty acid methyl esters

Ru-Sn/Al2O3 catalysts with different Sn loadings were prepared by the coimpregnation method. Several characterization techniques such as TPR, pyridine TPD and catalytic tests for dehydrogenation and hydrogenolysis were used to evaluate and compare such catalysts. TPR results indicate that Sn is deposited both onto the support and as species strongly interacting with Ru. Such non selective deposition modifies the acid and metallic functions of the catalysts. Both total acidity and acid strength distribution are affected: total acidity decreases and new sites of lower acid strength are created. Both dehydrogenating and hydrogenolytic activities are strongly diminished by the addition of Sn. Results of catalytic tests for methyl oleate hydrogenation indicate that methyl stearate is the main product, with only minute amounts of oleyl alcohol produced, and that the addition of Sn diminishes the hydrogenation activity.

Steroidal and phenolic compounds from Sidastrum paniculatum (L.) Fryxell and evaluation of cytotoxic and anti-inflammatory activities

Sidastrum paniculatum (L.) Fryxell belongs to the family Malvaceae and is popularly known as "malva roxa" or "malvavisco". The phytochemical study of the hexane, CHCl3 and EtOAc phases from the crude ethanol extract of S. paniculatum led to the isolation of six compounds: a mixture of β-sitosterol and stigmasterol, 4-methoxy-3-hydroxybenzoic acid, 4-methoxy-3-hydroxybenzaldehyde, N-trans-feruloyltyramine and kaempferol-3-O-β-D-(6''-E-p -coumaroyl) glucoside. The structural identification of the compounds was made on the basis of spectroscopic methods such as IR, ¹H and 13C NMR with the aid of including two-dimensional techniques, besides comparison with literature data. The β-sitosterol and stigmasterol mixture showed a significant anti-inflammatory activity.