Search results for "relation"

2020

Arts-based practices can support sustainability, combined with research that points out needs for intervention. We practiced environmental sensitivity and dialogic art with fifth-grade school pupil...

Synthesis of 8-aminomorphans with high KOR affinity

2021

2-Azabicyclo[3.3.1]nonanes (morphans) with a (3,4-dichlorophenyl)acetyl group at 2-position and a pyrrolidino moiety at 8-position were designed as conformationally restricted analogs of piperidine-based KOR agonists. The synthesis started with 4-oxopiperidine-2-carboxylic acid comprising 13 reaction steps. At first the ketone 10 was transformed into diester 7 bearing a propionate side chain. Dieckmann condensation of diester 7 to afford bicyclic enolester 14 and subsequent Krapcho deethoxycarbonylation represent the key steps of the synthesis. The enantiomeric pyrrolidines (1S,5R,8R)-5a and (1R,5S,8S)-5a were separated by chiral HPLC. The eutomer (1S,5R,8R)-5a showed high KOR affinity (K-i…

Direct synthesis of C3-mono-functionalized oxindoles from N-unprotected 2-oxindole and their antileishmanial activity.

2014

A novel approach for the synthesis of unprecedented C3-mono-functionalized indolin-2-ones is reported, starting from 2-oxindole and chalcones. The reactions proceed regioselectively under mild conditions, without di- and tri-alkylated side products. The new compounds have been evaluated in vitro for their antiproliferative effects against the protozoan Leishmania infantum. Interestingly, they appear able to kill L. infantum promastigotes and amastigotes, without significant cytotoxic effects.

The pyrrole moiety as a template for COX-1/COX-2 inhibitors

2000

Aroyl- and thiophene-substituted pyrrole derivatives have been synthesized as a new class of COX-1/COX-2 inhibitors. The inhibition of COX-1 was evaluated in a biological system using bovine PMNLs as the enzyme source, whereas LPS-stimulated human monocytes served as the enzyme source for inducible COX-2. The determination of the concentration of arachidonic acid metabolites was performed by HPLC for COX-1 and RIA for COX-2. Variation of the substitution pattern led to a series of active compounds which showed inhibition for COX-1 and COX-2. Structural requirements for the development of COX-1/COX-2 inhibitors are discussed.

Atom- and Bond-Based 2D TOMOCOMD-CARDD Approach and Ligand-Based Virtual Screening for the Drug Discovery of New Tyrosinase Inhibitors

2008

Two-dimensional atom- and bond-based TOMOCOMD-CARDD descriptors and linear discriminant analysis (LDA) are used in this report to perform a quantitative structure-activity relationship (QSAR) study of tyrosinase-inhibitory activity. A database of inhibitors of the enzyme is collected for this study, within 246 highly dissimilar molecules presenting antityrosinase activity. In total, 7 discriminant functions are obtained by using the whole set of atom- and bond-based 2D indices. All the LDA-based QSAR models show accuracies above 90% in the training set and values of the Matthews correlation coefficient (C) varying from 0.85 to 0.90. The external validation set shows globally good classifica…

Las representaciones del saber académico: Aportaciones desde la Geografía Escolar

2019

When we talk with basic education´s teachers there is an impression in the case of learning Social Sciences, and Geography in particular that these sciences are not useful for the explanation of socio-environmental and daily problems. In this research, improvement proposals are sought so that students are motivated to learn about these problems. Based on two case studies such as flood risks (and their relationship with climate change) and the problems of the rural areas, the possibilities of combining motivation for learning close to personal emotions and with their own rigor have been explored of the conceptual explanation. To validate these results, quantitative and qualitative research t…

El rol del modelo de las competencias en la reconfiguración meritocrática de las pautas de negociación salarial en empresas argentinas: continuidades…

2020

The development of new models of work organization and the complementary advance of flexible guidelines for the use of the labor force had as a correlate a profound change in techniques for the evaluation of workers. Thus, the typical model of Fordism, based on qualifications, was replaced by a different one based on competencies, whereby the strong relationship of the former was abandoned with the determination of the technical knowledge required for each job to move to a system which the priority is placed in the individual attitude. The consequent individualization of performance evaluations can lead to a possible loss of objectivity. In this article we develop a theoretical comparison b…

Associations of nutrition and body composition with cardiovascular disease risk factors in soldiers during a 6-month deployment

2020

Objectives This observational follow-up study investigated the associations of nutrition and body composition with cardiovascular disease (CVD) risk factors, including pro-inflammatory biomarkers, in soldiers during a 6-month deployment. Material and Methods Thirty-five male soldiers were assessed at months 0, 3 and 6, and their parameters, i.e., M±SD, were as follows: age 30.0±8.7 years, height 179±6 cm, and BMI 24.2±2.5 kg/m 2 . Three-day food diaries were used for monitoring macronutrient intake. Body composition was estimated using bioimpedance. Fasting blood samples for lipids and pro-inflammatory biomarkers were collected, and blood pressure measurements were performed. Results Carboh…

Slaves in Roman Society

2011

Sixfold coordinated phosphorus by oxygen in AlPO4 quartz homeotype under high pressure.

2007

International audience; AlPO4 belongs to the berlinite quartz homeotype family, which has been the subject of intense high pressure research triggered by the supposed existence of reversible pressure induced amorphization. New x-ray diffraction experiments, complemented with ab initio calculations, demonstrate the existence of two high pressure crystalline polymorphs and show that AlPO4 share the same two stage densification mechanism as silica. In first place a compact hexagonal sublattice of oxygen atoms is formed. In a second step the cations redistribute in the interstices giving rise to a monoclinic distorted CaCl2 phase. The most outstanding feature of the new phase is that phosphorou…