1,720,962 research outputs found
Synthesis of amides from aldehydes and amines via C-H bond activation and discovery and development of novel and selective carbonic anhydrase inhibitors
Full text linkThis doctoral dissertation consists of two chapters.In the first chapter is described the methodology developed for the synthesis of amides from aldehydes and amines by activating the aldehyde C-H bond. The technique involves the formation of N-chloro amine in situ, without being isolated from the reaction mixture, to which is then added the aldehyde. The two reagents in the presence of TBHP and Cu(OAc)2, forming the new CN bond. The method allowed to synthesize amides variously substituted in good yields.In the second chapter is detailed a project focused on the development of new original and selective carbonic anhydrases inhibitors. This chapter is divided into four topics which include a) the application of the click chemistry as a powerful synthetic approach for the generation of sulfonamide-based inhibitors; b) the synthesis of a set of derivatives belonging to a previously indentified hit compound bearing the trifluorodihydroxypropanone moiety, and the strategy adopted for its biological optimization; c) the design and development of novel pyrazole-carboxylic acids derived from a previously identified lead compound, as well as its pharmacobiological optimization; d) the synthesis of potential carbonic anhydrase inhibitors carrying a benzoxaborole scaffold
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe 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
Carbonic Anhydrase I
No full textAlthough carbonic anhydrase I (CA I) is one of the first CA isoforms discovered, its physiological and pathological functions are still poorly understood. Moreover, its role as a putative pharmacological target has not been validated yet. However, recent evidences highlighted that expression of CA I is involved in several diseases, and therefore the development of selective CA I modulators is expected. Structural and biological data are now available for this isozyme, and this information can be useful in the drug discovery process. To date, a plethora of potent CA inhibitors/activators have been identified, but only a few of them have demonstrated to be specific ligands of the CA I isoform. This chapter focuses on the structure and functions of CA I, with particular emphasis on its potential as a suitable drug target
Variations on the Author
Full text link“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
Full text linkWe 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
Dispelling the Myths Behind First-author Citation Counts
Full text linkWe conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
koamabayili/VECTRON-author-checklist: VECTRON author checklist
No full textWe have done our best to complete the author checklist relating to the use of animals in the hut study. Note that the objective for the hut study was to evaluate the IRS treatment applications for residual efficacy against Anopheles mosquitoes, including the local An. coluzzii mosquito population. Cows were only used to attract mosquitoes into the huts and no tests were carried out directly on the cows. The author checklist is intended for use with studies where experiments are carried out on animals, which is why we have had such difficulty in completing this for the hut study, as many of the questions do not relate to how the cows were used
Searching for novel carbonic anhydrase inhibitors: from virtual screening to the lab bench
Full text linkCarbonic Anhydrases (CAs) are zinc metalloenzymes that catalyze the reversible hydration of carbon dioxide to bicarbonate both in prokaryotes and eukaryotes. In this context, Computer Aided Drug Design strategies have emerged as powerful tools in the modern drug discovery paradigm. In particular, using ligand- and pharmacophore-based virtual screening approaches, we identified novel chemical entities with original chemotypes, that showed an interesting and selective inhibitory activity in nanomolar/low micromolar range toward CA I and CAII, isoforms.Herein, we present the hit-to-lead optimization process for these prototypes
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