Pyrazolo-triazolo-pyrimidines as adenosine receptor antagonists: A complete structure–activity profile

In the last 5 years, many efforts have been conducted searching potent and selective human A3 adenosine antagonists. In this field several different classes of compounds, possessing very good affinity (nM range) and with a broad range of selectivity, have been proposed. Recently, our group synthesized a new series of pyrazolo-triazolo-pyrimidines bearing different substitutions at the N5 and N8 positions, which have been described as highly potent and selective human A3 adenosine receptor antagonists. The present review summarizes available data and provides an overview of the structure–activity relationships found for this class of human A3 adenosine receptor antagonists

Predicting human eye fixations via an LSTM-Based saliency attentive model

Data-driven saliency has recently gained a lot of attention thanks to the use of convolutional neural networks for predicting gaze fixations. In this paper, we go beyond standard approaches to saliency prediction, in which gaze maps are computed with a feed-forward network, and present a novel model which can predict accurate saliency maps by incorporating neural attentive mechanisms. The core of our solution is a convolutional long short-term memory that focuses on the most salient regions of the input image to iteratively refine the predicted saliency map. In addition, to tackle the center bias typical of human eye fixations, our model can learn a set of prior maps generated with Gaussian functions. We show, through an extensive evaluation, that the proposed architecture outperforms the current state-of-the-art on public saliency prediction datasets. We further study the contribution of each key component to demonstrate their robustness on different scenarios

Sensitivity to damage imperfection for multileaf masonry walls based on vibrational analyses

Damage-imperfection indicators based on variation of dynamic parameters allow to identify the intrinsic discontinuity and the damage of structures. Here, the structural health monitoring through the vibration-based approach has been carried out by two steps on three different multileaf masonry specimens (full infill, damaged infill, and strengthened infill) subjected to uniaxial compressive load. In the first step, the characterization of initial conditions based on the investigation of the intrinsic discontinuity and the manufacturing imperfections has been done. In this phase, the detection, localization, assessment, and prediction of damage have been given by the comparison between the experimental and numerical modal data calculated by the commercial finite element code. Subsequently, in the second step, starting from the identification of undamaged condition, the damage effects on changes of the dynamic parameters have been recorded. As well known, the incoherent response between the leaves is related to frequency values, damping ratios, and modal shapes

Shot, scene and keyframe ordering for interactive video re-use

This paper presents a complete system for shot and scene detection in broadcast videos, as well as a method to select the best representative key-frames, which could be used in new interactive interfaces for accessing large collections of edited videos. The final goal is to enable an improved access to video footage and the re-use of video content with the direct management of user-selected video-clips

Identification of Contradictory Patterns in Experimental Datasets for the Development of Models for Electrical Cables Diagnostics

International audienceThe state of health of an electrical cable may be difficult to know, without destructive or very expensive tests. To overcome this, partial discharge (PD) measurements have been proposed as a relatively economic and simple-to-apply experimental technique for retrieving information on the state of health of an electrical cable. The retrieval is based on a relationship between PD measurements and the health of the cable. Given the difficulties in capturing such relationship by analytical models, empirical modeling techniques based on experimental data have been propounded. In this view, a set of PD measurements have been collected by Enea Ricerca sul Sistema Elettrico-ERSE during past campaigns, for building a diagnostic system of electrical cable health state. These experimental data may contain contradictory information which remarkably reduces the performance of the state classifier, if not a priori identified and possibly corrected. In the present paper, a novel technique based on the Adaboost algorithm is proposed for identifying contradictory PD patterns within an a priori analysis aimed at improving the diagnostic performance. Adaboost is a bootstrap-inspired, ensemble-based algorithm which has been effectively used for addressing classification problems

Beneficial effects of bunch-zone late defoliations and shoot positioning on berry composition and colour components of wines undergoing aging in an organically-managed and rainfed Sangiovese vineyard

n the context of climate change, where high temperatures are frequent in the first phases of ripening, protecting grapevine bunches from solar radiation is essential for preserving berry composition and wine colour. The effects of bunch-zone late defoliations (DEFs) and “semi-ballerina” shoot positioning (SB) on vine physiology and grape and wine quality of organic cv. Sangiovese wines during storage were assessed in two contrasting seasons (2013 and 2014). The treatments altered neither vine physiology (leaf photosynthetic activity and stomatal conductance, stem water potential) nor vine phenology, yield, budburst and fruitfulness. Defoliations imposed at post-veraison (DEF I) and pre-harvest (DEF II), but not shoot positioning imposed at post-veraison, enhanced the concentration of berry skin flavonols at harvest, compared to an untreated control. Late defoliations and SB did not change berry weight, anthocyanins, soluble solids, pH or titratable acidity at harvest. The severity of Botrytis bunch rot was assessed in both seasons. In 2013, it was negligible regardless of the treatment. In 2014 (characterised by higher rainfall and lower average temperatures than in 2013), late defoliations (DEF I and DEF II), especially DEF I, and SB to a minor extent, limited the severity of Botrytis bunch rot. The oenological benefits of late defoliations and shoot positioning were observed during wine storage. These canopy management practices positively influenced wine components (polymeric pigments; namely short polymeric pigments) that might have a marked effect on the final colour intensity, without altering the basic chemical characteristics of the wine. When choosing the timing for carrying out defoliation in order to improve grape quality and bunch rot containment, the meteorological conditions should be properly considered. Our results may contribute to providing further recommendations for canopy management for grape growers who produce organic Sangiovese wines that undergo aging

Structural investigation of the Rh(110)-c(2x2)-CN phase

The Rh(110)-c(2x2)-CN phase has been examined by means of scanning tunneling microscopy (STM) and full dynamical low-energy electron diffraction (LEED). From STM large c(2x2) domains are observed. The detailed LEED-IV structural analysis indicates that CN is located in the grooves of the (110) surface, approximately atop second layer rhodium atoms. The CN molecules lie almost flat with their bond axes oriented perpendicular to the rhodium troughs. An outward relaxation of the first substrate interlayer distance and a strong buckling of the second Rh layer are induced by CN adsorption. Calculated and experimental intensity curves are in good agreement. An exhaustive set of other possible adsorption sites and configurations was tested and excluded on the basis of reliability-factor analysis