1,721,138 research outputs found
Structure-Based Design, Solid Phase Synthesis and SAFIR of New Dual Binding Site Acetylcholinesterase (AChE) Inhibitors.
No full textDesign of multiple-target anticancer agents: a daunting challenge for the medicinal chemist
No full textImproved Fluorimetric Method for a Medium-Throughput Screening of Inhibitors of Beta-amyloid Aggregation: Application to Glycopeptide antibiotics and Quinone Derivatives
No full textMonoamine Oxidase Inhibition for the Treatment of Neurodegenerative Diseases: Rationale, Assay Methodologies, and Reference Compounds
No full textMonoamine oxidases (MAOs) A and B are key enzymes involved in the metabolism of amine neurotransmitters as well as exogenous amine-containing substances. Since their characterization in the 1960s, they represent a pharmacological target for the discovery of small molecular inhibitors, especially as antidepressants and antiparkinsonian drugs. The development of in vitro/in vivo assays has paralleled such interest allowing the setup of fast and reliable screening methods herein described. Hence, a huge number of potent and selective inhibitors have been discovered, although only in some cases reaching the pharmaceutical market. A renewed interest has emerged with the so-called multitarget approach, combining multiple biological activities in a single molecular entity, speeding up the screening of MAO inhibitors endowed with additional activities for the treatment of neurodegenerative diseases
Improved fluorimetric method for a MTS of inhibitors of beta-amyloid aggregation: application to glycopeptide antibiotics and quinones derivatives
No full textSydnone: Synthesis, Reactivity and Biological Activities
No full text: Sydnones are among the most well-known mesoionic compounds. Since their synthesis in 1935 by Earl and Mecknay, numerous researches have shown that the chemical behavior, physical and biological properties of sydnones make them among the most useful compounds in organic chemistry. Sydnones undergo thermal 1,3-dipolar cycloaddition reaction with dipolarophiles (alkynes or alkenes) to give exclusively derivatives containing a pyrazole moiety exhibiting numerous applications such as pharmaceuticals and agrochemicals. However, the sydnone cycloaddition reaction with alkynes requires harsh conditions like high temperatures and long reaction times giving poor regioselectivity on the resulting products. To overcome these constraints, new reactions named CuSAC (Copper-Catalyzed Sydnone-Alkyne Cycloaddition) and SPSAC (Strain-Promoted Sydnone-Alkyne Cycloaddition) and have been developed, leading to pyrazoles with interesting constant kinetics
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
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