1,721,041 research outputs found
NMR data of pyrazole derivatives as GSK-3beta inhibitors
No full textTwo sets of pyrazole-based derivatives (1a-k and 2-5 a-c) have been designed and synthesized by linking the privileged pyrazole scaffold with different amide side chains, in order to obtain inhibitors of GSK-3β enzyme. The compounds showed also chelating properties towards toxic metals. The dataset contains the free induction decay (fid) of 1H and 13C NMR spectra registered on a Bruker spectrometer working at 600 MHz and at 150 MHz of the new compounds and the corresponding jdx format files
Farmaci cardiaci
No full textLe patologie cardiovascolari, di cui l’insufficienza cardiaca, le varie forme di aritmia, l’angina pectoris e l’ipertensione costituiscono le più comuni, rappresentano a tutt’oggi la principale causa di mortalità nei paesi industrializzati. Fumo, obesità e stress, riconducibili ad un errato stile di vita, rappresentano rilevanti fattori di rischio, ma anche stati patologici come diabete, alterazioni del bilancio lipidico e dell’attività tiroidea possono contribuire alla loro insorgenza.
La regolazione fisiologica del sistema cardiovascolare è molto complessa e dipendente da fattori neuronali, umorali e strutturali. Inoltre, la contrattilità cardiaca stessa si verifica con un meccanismo automatico atipico rispetto alla contrazione di altri organi, e la maggior parte dei farmaci cardiaci agisce sugli eventi elettrofisiologici alla base dell’accoppiamento eccito-contrattile del cuore. Insufficienza cardiaca, aritmia e angina pectoris possono essere considerate le cardiopatie più diffuse. Il capitolo tratterà pertanto i farmaci attualmente impiegati per il trattamento di questi disturbi esaminandone meccanismo d’azione, relazioni struttura attività e procedure sintetiche
Data from molecular mechanism investigation on new purposely designed hybrid compounds to inhibit NDH-2 enzyme of P. falciparum and S. aureus
No full textA series of hybrid compounds has been designed and synthesized by linking the pharmacophore of the antimalarial drug chloroquine with the phenothiazine core. The dataset contains the free induction decay (fid) of 1H and 13C NMR spectra registered on a Bruker spectrometer working at 600 MHz and at 150 MHz of the new compounds and the optical density measurements of the microbial and cellular growths of the experimental model systems treated with the hybrid compounds
Tackling Alzheimer's Disease with Existing Drugs:A Promising Strategy for Bypassing Obstacles
Full text linkThe unmet need for the development of effective drugs to treat Alzheimer's disease has been steadily growing, representing a major challenge in drug discovery. In this con-text, drug repurposing, namely the identification of novel therapeutic indications for approved or investigational compounds, can be seen as an attractive attempt to obtain new medications reducing both the time and the economic burden usually required for research and development programs. In the last years, several classes of drugs have evidenced promising beneficial effects in neurodegenerative diseases, and for some of them, preliminary clinical trials have been started. This review aims to illustrate some of the most recent examples of drugs reprofiled for Alzheimer’s disease, considering not only the finding of new uses for existing drugs but also the new hypotheses on disease pathogenesis that could promote previ-ously unconsidered therapeutic regimens. Moreover, some examples of structural modifica-tions performed on existing drugs in order to obtain multifunctional compounds will also be described
Cardiovascular Profile of Xanthone-Based 1,4 Dihydropyridines Bearing a Lidoflazine Pharmacophore Fragment
Full text linkAs a follow-up to our previous studies on differently substituted 1,4-dihydropyridines endowed with a peculiar cardiac selectivity, in this paper, a small series of hybrid compounds bearing the pharmacophore fragment of lidoflazine in position 2 or 3 on a 4-(xanthen-9-one)-dihydropyridine core was reported. Lidoflazine was selected due to our promising previously reported data, and the xanthen-9-one substituent was introduced in position 4 of the dihydropyridine scaffold based on the cardiac selectivity observed in several of our studies. The new hybrid compounds were tested to assess cardiac and vascular activities, and the data were evaluated in comparison with those previously obtained for 4-(xanthen-9-one)-dihydropyridines and lidoflazine⁻nifedipine hybrid compounds. The functional studies indicated an interesting peculiar selectivity for the cardiac parameter inotropy, in particular when the lidoflazine fragment was introduced in position 2 of the dihydropyridine scaffold (4a⁻e), and thus a possible preferential binding with the Cav 1.2 isoform of l-type calcium channels, which are mainly involved in cardiac contractility
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
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
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