N-acylbenzimidazoles as selective Acylators of the catalytic cystein of the coronavirus 3CL protease.

The 3CL protease (3CL, M) plays a key role in the replication of the SARS-CoV-2 and was validated as therapeutic target by the development and approval of specific antiviral drugs (nirmatrelvir, ensitrelvir), inhibitors of this protease. Moreover, its high conservation within the coronavirus family renders it an attractive therapeutic target for the development of anti-coronavirus compounds with broad spectrum activity to control COVID-19 and future coronavirus diseases. Here we report on the design, synthesis and structure-activity relationships of a new series of small covalent reversible inhibitors of the SARS-CoV-2 3CL.

Novel dithiocarbamates selectively inhibit 3CL protease of SARS-CoV-2 and other coronaviruses.

Since end of 2019, the global and unprecedented outbreak caused by the coronavirus SARS-CoV-2 led to dramatic numbers of infections and deaths worldwide. SARS-CoV-2 produces two large viral polyproteins which are cleaved by two cysteine proteases encoded by the virus, the 3CL protease (3CL) and the papain-like protease, to generate non-structural proteins essential for the virus life cycle. Both proteases are recognized as promising drug targets for the development of anti-coronavirus chemotherapy.

Tricyclic SpiroLactams Kill Mycobacteria In Vitro and In Vivo by Inhibiting Type II NADH Dehydrogenases.

It is critical that novel classes of antituberculosis drugs are developed to combat the increasing burden of infections by multidrug-resistant strains. To identify such a novel class of antibiotics, a chemical library of unique 3-D bioinspired molecules was explored revealing a promising, mycobacterium specific Tricyclic SpiroLactam (TriSLa) hit. Chemical optimization of the TriSLa scaffold delivered potent analogues with nanomolar activity against replicating and nonreplicating .

A new blind color watermarking based on a psychovisual model.

In this paper, we address the problem of the use of a human visual system (HVS) model to improve watermark invisibility. We propose a new color watermarking algorithm based on the minimization of the perception of color differences. This algorithm is based on a psychovisual model of the dynamics of cone photoreceptors.

Experimental determination of pesticide processing factors during extraction of seed oils.

Processing Factors (PFs) reflect the concentration or dilution of pesticide residues resulting from food processing. PFs are key elements to demonstrate the compliance of processed foods with Maximum residue levels (MRLs) as set by Regulation 396/2005. While efforts have been made by the European Food Safety Authority (EFSA) and by national authorities to compile PFs from processing studies, such PFs are not available for all pesticides/processed product combinations.

Phase estimation of a 2D fringe pattern using a monogenic-based multiscale analysis.

In this paper, a multiscale monogenic analysis is applied to 2D interference fringe patterns. The monogenic signal was originally developed as a 2D generalization of the well-known analytic signal in the 1D case. The analytic and monogenic tools are both useful to extract phase information, which can then be directly linked with physical quantities.

Pelleting and extrusion can ameliorate negative effects of toasting of rapeseed meal on protein digestibility in growing pigs.

Toasting time (TT) of rapeseed meal (RSM), the diet processing (DP) method and the interaction between both on the apparent CP digestion along the gastrointestinal tract and the apparent ileal digestibility (AID) of amino acids of growing pigs were investigated. The experiment consisted of a 3×3 factorial design of TT of RSM (0, 60 and 120 min) and DP method (mash, pelleting and extrusion). In total, 81 boars with a starting BW of 20 kg were euthanized 4 h after their last feeding.

Characterization of Color Images with Multiscale Monogenic Maxima.

Can we build a feature-based analysis that fully characterizes images? The literature answers with edge-based reconstruction methods inspired by Marr's paradigm but limited to the greyscale case. This paper studies the color case. A new sparse representation is carried out with the monogenic concept and the Mallat-Zhong wavelet maxima method.

Investigations of the nutritive value of meals of double-low rapeseed and its influence on growth performance of broiler chickens.

Four experiments were carried out to study the possible differences in metabolizable energy (ME) of meals (RSM) or expeller meals (RSE) from double-low rapeseed (Expt. 1), the influence of processing on ME (Expt. 2) and on relative phosphorus (P) bioavailability (Expt.

Effects of Toasting Time on Digestive Hydrolysis of Soluble and Insoluble 00-Rapeseed Meal Proteins.

Thermal damage to proteins can reduce their nutritional value. The effects of toasting time on the kinetics of hydrolysis, the resulting molecular weight distribution of 00-rapeseed meal (RSM) and the soluble and insoluble protein fractions separated from the RSM were studied. Hydrolysis was performed with pancreatic proteases to represent protein digestibility.

Physical and chemical changes of rapeseed meal proteins during toasting and their effects on digestibility.

Background: Toasting during the production of rapeseed meal (RSM) decreases ileal crude protein (CP) and amino acid (AA) digestibility. The mechanisms that determine the decrease in digestibility have not been fully elucidated. A high protein quality, low-denatured, RSM was produced and toasted up to 120 min, with samples taken every 20 min.

Effect of the desolventizing/toasting process on chemical composition and protein quality of rapeseed meal.

Background: During processing in a desolventizer/toaster (DT), rapeseed meal (RSM) is heated to evaporate the hexane and to reduce the level of heat-labile anti-nutritional factors such as glucosinolates (GSL). However, excessive heat treatment may reduce amino acid (AA) content in addition to lower AA digestibility and availability in RSM. The objective of the present study was to produce from one batch of a 00-rapeseed variety (17 μmol GSL/g dry matter (DM), seed grade quality) five differently processed RSM under standardized and defined conditions in a pilot plant, and to determine the impact of these different treatments on protein solubility and chemical composition, in particular with regard to contents of AA including reactive Lys (rLys) and levels of total and individual GSL.

Ultrasound induced green solvent extraction of oil from oleaginous seeds.

Ultrasound-assisted extraction of rapeseed oil was investigated and compared with conventional extraction for energy efficiency, throughput time, extraction yield, cleanness, processing cost and product quality. A multivariate study enabled us to define optimal parameters (7.7 W/cm(2) for ultrasonic power intensity, 40 °C for processing temperature, and a solid/liquid ratio of 1/15) for ultrasound-assisted extraction of oil from oilseeds to maximize lipid yield while reducing solvent consumption and extraction time using response surface methodology (RSM) with a three-variable central composite design (CCD).

Alternative bio-based solvents for extraction of fat and oils: solubility prediction, global yield, extraction kinetics, chemical composition and cost of manufacturing.

The present study was designed to evaluate the performance of alternative bio-based solvents, more especially 2-methyltetrahydrofuran, obtained from crop's byproducts for the substitution of petroleum solvents such as hexane in the extraction of fat and oils for food (edible oil) and non-food (bio fuel) applications. First a solvent selection as well as an evaluation of the performance was made with Hansen Solubility Parameters and the COnductor-like Screening MOdel for Realistic Solvation (COSMO-RS) simulations. Experiments were performed on rapeseed oil extraction at laboratory and pilot plant scale for the determination of lipid yields, extraction kinetics, diffusion modeling, and complete lipid composition in term of fatty acids and micronutrients (sterols, tocopherols and tocotrienols).

Diagnosis and management of idiopathic pulmonary fibrosis: French practical guidelines.

Idiopathic pulmonary fibrosis (IPF) is the most frequent chronic idiopathic interstitial pneumonia in adults. The management of rare diseases in France has been organised by a national plan for rare diseases, which endorsed a network of expert centres for rare diseases throughout France. This article is an overview of the executive summary of the French guidelines for the management of IPF, an initiative that emanated from the French National Reference Centre and the Network of Regional Competence Centres for Rare Lung Diseases.