New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives

A library of isoquinolinone and azepanone derivatives were screened for both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activity. The strategy adopted included (a) in vitro biological assays, against eel AChE (EeAChE) and equine serum BuChE (EqBuChE) in order to determine the compounds IC50 and their dose-response activity, consolidated by (b) molecular docking studies to evaluate the docking poses and interatomic interactions in the case of the hit compounds, validated by STD-NMR studies. Compound (1f) was identified as one of these hits with an IC50 of 89.5 mu M for EeAChE and 153.8 mu M for EqBuChE, (2a) was identified as a second hit with an IC50 of 108.4 mu M (EeAChE) and 277.8 mu M (EqBuChE). In order to gain insights into the binding mode and principle active site interactions of these molecules, (R)-(1f) along with 3 other analogues (also as the R-enantiomer) were docked into both RhAChE and hBuChE models. Galantamine was used as the benchmark. The docking study was validated by performing an STD-NMR study of (1f) with EeAChE using galantamine as the benchmark.

A LEITURA NA BIBLIOTECA PÚBLICA DE ÉVORA: UM CONTRIBUTO PARA A HISTÓRIA DA LEITURA EM PORTUGAL (1887-1921)

A Biblioteca Pública de Évora é uma das mais importantes bibliotecas patrimoniais de Portugal, quer pela sua colecção quer por ter sido uma das primeiras bibliotecas a abrir as portas aos leitores. Neste trabalho analisam-se os dados sobre a leitura na Biblioteca Pública de Évora, entre 1887-1921, em particular o número de lei- tores em cada ano, os livros requisitados, as temáticas mais populares, a leitura de jornais e a comparação entre a leitura pública e a alfabetização da população. Como fontes utilizam-se os dados publicados pelo Anuário Estatístico de Portugal, os livros de registo de leitores e visitantes, os relatórios dos bibliotecários e verbetes de leitura. Esta análise tem como objectivo traçar o perfil do leitor da Biblioteca Pública de Évora e contribuir para a caracterização do público leitor em Portugal na transição do século XIX para o século XX.Abstract: The Public Library of Évora is one of the most important heritage libraries of Portugal, both for its collection either by being one of the first libraries to open the doors to readers. This paper analyzes the data on reading at Public Library of Évora, between 1887-1921, in particular the number of readers in each year, the required books, the most popular themes, reading newspapers and the comparison between the public reading and literacy of the population. It is use as sources the data published by the Statistical Yearbook of Portugal, readers and visitors registration books, reports from librarians and reading entries. This analysis aims to draw the profile of reader at the Public Library of Évora and contribute to the characterization of the reading public in Portugal in the transition of the nineteenth century to the twentieth century.

Content analysis model to analyze facets of social mission of public library on the Facebook and in the websites

In this paper we present the development and the implementation of a content analysis model for observing aspects relating to the social mission of the public library on Facebook pages and websites. The model is unique and it was developed from the literature. There were designed the four categories for analysis Generate social capital and social cohesion, Consolidate democracy and citizenship, Social and digital inclusion and Fighting illiteracies. The model enabled the collection and the analysis of data applied to a case study consisting of 99 Portuguese public libraries with Facebook page. With this model of content analysis we observed the facets of social mission and we read the actions with social facets on the Facebook page and in the websites of public libraries. At the end we discuss in parallel the results of observation of the Facebook of libraries and the websites. By reading the description of the actions of the social mission, the general conclusion and the most immediate is that 99 public libraries on Facebook and websites rarely publish social character actions, and the results are little satisfying. The Portuguese public libraries highlight substantially the actions in the category Generate social capital and social cohesion.