Relatório da prática de ensino supervisionada na área da especialização do Mestrado em ensino de Física e Qímica, na escola secundária/3 Rainha Santa Isabel

O presente relatório descreve o trabalho realizado por nós, no âmbito da Prática de Ensino Supervisionada (PES), no ano lectivo 2010-2011, na Escola Secundária Rainha Santa Isabel, Estremoz. Está dividido em cinco capítulos. No primeiro capítulo discutimos o currículo das disciplinas de Ciências Físico-Químicas e de Física e Química A, bem como os conteúdos inerentes às unidades curriculares. Neste capítulo faremos ainda a caracterização das turmas intervencionadas. No segundo capítulo é resumido o trabalho realizado com as turmas durante o ano e é abordada, criticamente, a avaliação das aprendizagens dos alunos. No terceiro capítulo é feita uma análise da prática de ensino, enquadrada no âmbito da Didáctica das Ciências e da Psicologia do Desenvolvimento. No quarto capítulo abordamos o modo de funcionamento da escola e apresentamos o trabalho extra-curricular desenvolvido em parceria com outros docentes. No quinto capítulo é feita uma reflexão crítica do trabalho por nós desenvolvido durante a PES; ABSTRACT:This report describes the work done by us under the Supervised Teaching Practice (STP), during the 2010-2011 school year, at Rainha Santa Isabel High School, Estremoz. It’s divided into five chapters. In the first chapter we discuss the curriculum of the disciplines of Physics and Chemistry Sciences and of Physics and Chemistry A, as well as the inherent content of the curricular units. In this chapter we will further the characterization of classes intervened. The second chapter summarizes the work done with the classes during the year, and addresses, according to a critical perspective, the assessment of student learning. The third chapter is an analysis of the teaching practice, framed within the Didactic Science and Developmental Psychology. In the fourth chapter is presented the operating mode of the school and the extracurricular work developed in partnership with other teachers. In the fifth chapter, discussions were held as a critical reflection of the work developed by us during the STP

In silico, NMR and pharmacological evaluation of an hydroxyoxindole cholinesterase inhibitor

From a screening study of various potential inhibitors for cholinesterases (ChEs), compound (rac)-1 (4-((3-hydroxy-2-oxo-3-phenylindolin-1-yl) methyl) piperidin-1-ium chloride) showed an IC50 of 18 μM for butyrylcholinesterase (BuChE). Herein we present a toxicological and pharmacological evaluation of (rac)-1 to determine its potential for use as an alternative ChE inhibitor for the treatment of Alzheimer’s disease. The strategy adopted included in vivo and ex vivo studies with mouse models, Molecular Modelling and Saturation Transfer Difference (STD) NMR studies. Preliminary molecular docking studies were conducted with both (R) and (S)-1 with acetylcholinesterase (AChE) and BuChE, prior to advancing to the mouse model, and indeed favorable interactions were observed, with (R)-1 showing the best binding with AChE and (S)-1 with BuChE. STD-NMR studies were used to successfully validate these results. Toxicological studies were also conducted using the Artemia salina model, with donepezil as reference. It was found that in the in vivo mouse studies that (rac)-1 presented a slightly better inhibition of AChE (0.096 µmol.min−1.mg−1) than donepezil (0.112 µmol.min−1.mg−1) and the same level of inhibition for BuChE as donepezil (0.014 µmol.min−1.mg−1)

Pharmacological evaluation and SAR studies of oxindole derivatives as cholinesterase inhibitors

From a screening study of various potential inhibitors for cholinesterases (ChEs), compound (rac)-1(4-((3-hydroxy-2-oxo-3-phenylindolin-1-yl)methyl) piperidin-1-ium chloride) showed an IC50 of 18 mu M for butyrylcholinesterase (BuChE). Herein we present a toxicological and pharmacological evaluation of (rac)-1 to determine its potential for use as an alternative ChE inhibitor for the treatment of Alzheimer's disease. The strategy adopted included in vivo and ex vivo studies with mouse models, Molecular Modelling and Saturation Transfer Difference (STD) NMR studies. Preliminary molecular docking studies were conducted with both (R) and (S)-1 with acetylcholinesterase (AChE) and BuChE, prior to advancing to the mouse model, and indeed favorable interactions were observed, with (R)-1 showing the best binding with AChE and (S)-1 with BuChE. STD-NMR studies were used to successfully validate these results. Toxicological studies were also conducted using the Artemia salina model, with donepezil as reference. It was found that in the in vivo mouse studies that (rac)-1 presented a slightly better inhibition of AChE (0.096 mu mol.min(-1).mg(-1)) than donepezil (0.112 mu mol.min(-1).mg(-1)) and the same level of inhibition for BuChE as donepezil (0.014 mu mol.min(-1).mg(-1))