1,721,053 research outputs found

    Hybridization approach to drug discovery inhibiting Mycobacterium tuberculosis. An overview

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    Tuberculosis is one of the top 10 causes of death worldwide and the leading cause of death from a single infectious agent mainly due to Mycobacterium tuberculosis (MTB). Recently, clinical prognoses have worsened due to the emergence of multi-drug resistant (MDR) and extensive-drug resistant (XDR) tuberculosis which lead to the need of new, efficient and safely drugs. Among the several strategies, polypharmacology could be considered one of the best solutions, in particular the multi-target directed ligands strategy (MTDLs), based on the synthesis of hybrid ligands acting against two targets of the pathogen. The framework strategy comprises linking, fusing and merging approaches to develop new chemical entities. With these premises, this review aims to provide an overview of recent hybridization approach, in medicinal chemistry, of the most recent and promising multitargeting antimycobacterial candidates

    Analisi Farmaceutica Qualitativa

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    Lo scopo di questo testo è quello di fornire un manuale di facile consultazione per tutti gli studenti dei corsi di laurea in Farmacia e in Chimica e Tecnologia Farmaceutiche, che frequentano un corso di analisi organica e/o inorganica qualitativa di sostanze farmaceutiche. Il manuale è ulteriormente rivolto a tutti coloro che hanno necessità di una guida che indirizzi in modo sistematico ad una rapida separazione di miscele e identificazione delle singole componenti senza l’ausilio di particolari tecniche strumentali. Questo, per esempio, è il caso dell’espletamento della prova di riconoscimento di farmaci incogniti prevista dall’esame di stato per l’abilitazione alla professione di farmacista. L’impostazione seguita nella stesura del testo è di tipo tradizionale. L’obiettivo principale del libro è quello di guidare il lettore attraverso un percorso analitico sistematico che, mediante una serie di operazioni sequenziali, consenta di riconoscere da prima la classe di appartenenza del farmaco incognito e successivamente la sua identificazione. La prima parte del testo illustra i principi chimici e fisici nonché tutte le operazioni pratiche e le apparecchiature più comunemente utilizzate per isolare un composto puro da una miscela (o miscuglio). Le tecniche descritte in questa parte del testo sono: estrazione con solvente, cristallizzazione, distillazione, cromatografia, evaporazione, filtrazione e centrifugazione

    New piperidine-based derivatives as sigma receptor ligands. Synthesis and pharmacological evaluation

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    The sigma receptor (σR) family has been considered mysterious for a long time. In fact, the σ2R subtype has been cloned only recently, revealing its identity as TMEM97, a NPC1-binding protein involved in cholesterol biosynthesis and implicated in the pathogenesis of cancer and neurologic disorders. With the aim of developing new chemical entities gifted with σR affinity, herein we report the design and synthesis of new piperidine-based alkylacetamide derivatives with mixed affinity towards both σ1 and σ2R subtypes

    Going Beyond Counting First Authors in Author Co-citation Analysis

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    The present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed

    Variations on the Author

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    “Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship

    Appropriate Similarity Measures for Author Cocitation Analysis

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    We provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
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