Search results for "very"

Discovery of a new class of sortase a transpeptidase inhibitors to tackle gram-positive pathogens: 2-(2-phenylhydrazinylidene)alkanoic acids and rela…

2016

A FRET-based random screening assay was used to generate hit compounds as sortase A inhibitors that allowed us to identify ethyl 3-oxo-2-(2-phenylhydrazinylidene)butanoate as an example of a new class of sortase A inhibitors. Other analogues were generated by changing the ethoxycarbonyl function for a carboxy, cyano or amide group, or introducing substituents in the phenyl ring of the ester and acid derivatives. The most active derivative found was 3-oxo-2-(2-(3,4dichlorophenyl)hydrazinylidene)butanoic acid (2b), showing an IC50 value of 50 µM. For a preliminary assessment of their antivirulence properties the new derivatives were tested for their antibiofilm activity. The most active compo…

Collaborative Design Rational and Social Creativity in Cultures of Participation

2011

The rise in social computing has facilitated a shift from consumer cultures, focused on producing finished media to be consumed passively, to cultures of participation, where people can access the means to participate actively in personally meaningful problems. These developments represent unique and fundamental opportunities and challenges for rethinking and reinventing design rationale and creativity, as people acclimate to taking part in computer-mediated conversations of issues and their solutions. Grounded in our long-term research exploring these topics, this paper articulates arguments, describes and discusses conceptual frameworks and system developments (in the context of three cas…

Synthesis and Structure Elucidation of Novel Spirooxindole Linked to Ferrocene and Triazole Systems via [3 + 2] Cycloaddition Reaction

2022

In the present work, a novel heterocyclic hybrid of a spirooxindole system was synthesized via the attachment of ferrocene and triazole motifs into an azomethine ylide by [3 + 2] cycloaddition reaction protocol. The X-ray structure of the heterocyclic hybrid (1″R,2″S,3R)-2″-(1-(3-chloro-4-fluorophenyl)-5-methyl-1H-1,2,3-triazole-4-carbonyl)-5-methyl-1″-(ferrocin-2-yl)-1″,2″,5″,6″,7″,7a″-hexahydrospiro[indoline-3,3″-pyrrolizin]-2-one revealed very well the expected structure, by using different analytical tools (FTIR and NMR spectroscopy). It crystallized in the triclinic-crystal system and the P-1-space group. The unit cell p…

Polymeric micelles containing squalenoyl chains for the delivery of drugs to the central nervous system

2011

Behind the scenes of artificial intelligence: a study of micro-work platforms in France

2019

Este artículo es una versión resumida del informe “Le Micro-travail en France. Derrière l’automatisation de nouvelles précarités au travail?» This article is a summarized version of the report "Le Micro-travail en France. Derrière l’automatisation de nouvelles précarités au travail?" .; International audience; Micro-work internet services allocate small, standardized tasks of data generation and annotation to crowds of providers. The outputs are mainly used to produce artificial intelligence solutions. It is an exemplary instance of the “platformization” of the economy, and of the transformations of labour that digital technologies bring about. To uncover the conditions under which micro-wo…

Variation of the Effect of Surface Acting on General Health and Need for Recovery Based on the Frequency of Interactions at Work: A Multi-Group Analy…

2022

Compared Binding Properties between Resveratrol and Other Polyphenols to Plasmatic Albumin: Consequences for the Health Protecting Effect of Dietary …

2014

International audience; Phytophenols are considered to have beneficial effects towards human physiology. They are food microcomponents with potent chemopreventive properties towards the most three frequent contemporary human diseases, e.g., cardiovascular alterations, cancer and neurodegenerative pathologies. Related to this, the plasmatic form and plasmatic level of plant polyphenols in the body circulation are crucial for their efficiency. Thus, determinations of the binding process of resveratrol and of common flavonoids produced by major edible plants, berries and fruits to plasma proteins are essential. The interactions between resveratrol and albumin, a major plasma protein, were comp…

Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of t…

2009

The biological importance of microtubules in mitosis and cell division makes them an interesting target for the development of anticancer agents. Small molecules such as benzo[b]furans are attractive as inhibitors of tubulin polymerization. Thus, a new class of inhibitors of tubulin polymerization based on the 2-(3′,4′,5′-trimethoxybenzoyl)-benzo[b]furan molecular skeleton, with electron-donating (Me, OMe or OH) or electron-withdrawing (F, Cl and Br) substituents on the benzene ring, was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization and cell cycle effects. Adding a methyl group at the C-3 position resulted in increased activity. The most prom…

How do health care services help and hinder recovery after a suicide attempt? A qualitative analysis of Finnish service user perspectives

2022

Background Suicide attempt survivors are at high risk of re-attempts and suicide death. Previous research has shown that service users’ experiences of post-attempt care are related to future treatment engagement and re-attempts. In-depth understanding of how current services meet service users’ needs in the period immediately following a suicide attempt is thus imperative for the development of more effective tertiary prevention practices in real-life health care systems. Method In this qualitative study, Finnish suicide attempt survivors’ experiences of and perspectives on mental health services were explored through a semi-structured interview. Participants were seven female and seven mal…

Titanocene Selenide Sulfides Revisited: Formation, Stabilities, and NMR Spectroscopic Properties

2019

[TiCp2S5] (phase A), [TiCp2Se5] (phase F), and five solid solutions of mixed titanocene selenide sulfides [TiCp2SexS5−x] (Cp = C5H5−) with the initial Se:S ranging from 1:4 to 4:1 (phases B–E) were prepared by reduction of elemental sulfur or selenium or their mixtures by lithium triethylhydridoborate in thf followed by the treatment with titanocene dichloride [TiCp2Cl2]. Their 77Se and 13C NMR spectra were recorded from the CS2 solution. The definite assignment of the 77Se NMR spectra was based on the PBE0/def2-TZVPP calculations of the 77Se chemical shifts and is supported by 13C NMR spectra of the samples. The following complexes in varying ratios were identified in the CS2 solutions of …