1,721,030 research outputs found
Synthetic Approach to Phenylalanine-Proline, and Tyrosine-Proline Hybrid Amino Acids
No full textSubstituted proline derivatives represent an important class of conformationally constrained amino acids. The combination of the structural properties of proline and the side-chain of another amino acid could help the development of peptidomimetics and SAR study of active compounds. The presence of a phenyl or a p-hydroxy-phenyl ring on the pyrrolidine ring could be considered as phenylalanine- or thyrosine-proline hybrids. These compounds have shown the potential to mimic natural occurring peptides and can activate or inhibit the respective receptor. This review will focus on the chemical strategy applied to synthesize these analogues. © 2016 Bentham Science Publishers
Synthetic strategies for lysine-proline chimeras: An overview
No full textProline-amino acid chimeras are conformationally rigid amino acid analogues, important in understanding the spatial requirements for receptor affinity and biological activity of natural amino acids and peptides. In medicinal chemistry, a great variety of lysine-proline chimeras was considered in light of the importance of their biological roles. In this review, we analyze the most relevant synthetic approaches to obtain lysine-proline chimeras
Il Progetto Value for Schools: Ricerca pedagogica e Learning Analytics per l’autovalutazione delle scuole
Full text linkIn the wake of the innovative thrusts of scholastic evaluation systems coming from the international and European context, as well as the development in this last decade of Learning Analytics (LA), as a new sector of Technology- Enhanced Learning (TEL), the scientific approach to educational research broadens its horizons and invites us to understand how Research, Technology, Pedagogy and Evaluation can/should constructively dialogue. In fact, in view of the sudden development of the LA, the need to connect the collection and analysis of data on school evaluation in direct synergy with the pedagogical and psychological principles of learning processes and the interpersonal dynamics activated in governance emerges more and more. The present study, starting from the political scenario and from the technological evolution mentioned above, aims to illustrate the pedagogical structure of the project “Valu.E for schools - Supporting school self-evaluation”, promoted by INVALSI, whose purpose is to “test and evaluate the effectiveness of different training models to support school self-evaluation activities.” It presents itself as an innovative heuristic purpose that opens up interesting and fertile spaces for dialogue between educational research, professional training and self-evaluation of schools.Sulla scia delle spinte innovative dei sistemi di valutazione scolastica provenienti dal contesto internazionale ed europeo, nonché dello sviluppo in questo ultimo decennio del Learning Analytics (LA), quale nuovo settore del Technology-Enhanced Learning (TEL), l’approccio scientifico alla ricerca educativa allarga i suoi orizzonti e ci invita a comprendere come Ricerca, Tecnologia, Pedagogia e Valutazione possano/debbano dialogare costruttivamente. A fronte del repentino sviluppo del LA emerge sempre più, infatti, la necessità di connettere la raccolta e l’analisi dei dati in ambito scolastico in diretta sinergia con i principi pedagogici e psicologici dei processi di apprendimento e alle dinamiche interpersonali attivate nella governance. Il presente studio, partendo dallo scenario politico e dall’evoluzione tecnologica su menzionati, ha l’obiettivo di illustrare l’impianto pedagogico del progetto “Valu.E for schools - Sostenere l’autovalutazione delle scuole”, promosso dall’INVALSI, la cui finalità è di “testare e valutare l’efficacia di modelli formativi diversi a supporto delle attività di autovalutazione delle scuole.” Esso si presenta come proposito euristico innovativo che apre interessanti e fertili spazi di dialogo tra ricerca educativa, formazione professionale e autovalutazione delle scuole
Stilbene derivatives as new perspective in antifungal medicinal chemistry
No full textThe high incidence and mortality of invasive fungal infections and serious drug resistance have become a global public health issue. There is an urgent need for alternative antimicrobials to control fungal infections and targeting it by antifungal substances from the natural sources represents a promising new strategy for the development of novel antifungal agents. Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a phytoalexin produced by plant species in response to environmental stress or pathogenic attacks. It has many known and potential therapeutic applications in human general homeostasis; it mediates a great number of biological responses relevant for human health such as anticancer, cardio and neuroprotective, antioxidant, and antimicrobial activities. Resveratrol is a natural antifungal agent, therefore it can be considered as a scaffold for designing structural relatives potentially capable of mediating more intense responses in a more specific way. Also, stilbenes produced by several plants may be useful lead structure for the chemical synthesis of antifungal. Their antifungal potential represents a useful solution to the drug resistance and side effect complications that occur after pharmacological treatment of infectious diseases. The purpose of this review is to present an overview on resveratrol derivatives, both natural and synthetic, with antifungal activity and summarize the chemical structure and the therapeutic versatility of stilbene-containing compounds
Blocking the Peroxisome Proliferator‐Activated Receptor (PPAR): An Overview
No full textPeroxisome proliferator-activated receptors (PPARs) have been studied extensively over the last few decades and have been assessed as molecular targets for the development of drugs against metabolic disorders. A rapid increase in understanding of the physiology and pharmacology of these receptors has occurred, together with the identification of novel chemical structures that are able to activate the various PPAR subtypes. More recent evidence suggests that moderate activation of these receptors could be favorable in pathological situations due to a decrease in the side effects brought about by PPAR agonists. PPAR partial agonists and antagonists are interesting tools that are currently used to better elucidate the biological processes modulated by this family of nuclear receptors. Herein we present an overview of the various molecular structures that are able to block each of the PPAR subtypes, with a focus on promising therapeutic applications
<i>N</i>-acylsulfonamides: Synthetic routes and biological potential in medicinal chemistry
No full textSulfonamide is a common structural motif in naturally occurring and synthetic medicinal compounds. The rising interest in sulfonamides and N-acyl derivatives is attested by the large number of drugs and lead compounds identified in last years, explored in different fields of medicinal chemistry and showing biological activity. Many acylsulfonamide derivatives were designed and synthesized as isosteres of carboxylic acids, being the characteristics of these functional groups very close. Starting from chemical routes to N-acylsulfonamides, this review explores compounds of pharmaceutical interest, developed as enzymatic inhibitors or targeting receptors
Sintesi di analoghi chirali del gemfibrozil 2,5,disostituiti a potenziale attività antiaggregante piastrinica
No full textDeterminazione della configurazione assoluta di acidi carbossilici a-sostituiti di interesse farmaceutico attraverso spettroscopia NMR
No full textDynamic kinetic resolution of α-bromoesters containing lactamides as chiral auxiliaries
No full textThe conversion of racemic α-bromobutanoic acid into the corresponding esters with amides of (S)-lactic acid as chiral auxiliaries was examinated. Displacement of the bromine with 4-chlorophenoxide, under suitable reaction conditions, was found to proceed with good to high diastereoselectivity to give 4-(chlorophenoxy)butanoyl esters. After hydrolysis, the (R)-enantiomer of antilipidemic 2-(4-chlorophenoxy)butanoic acid was obtained
PPAR-γ agonist GL516 reduces oxidative stress and apoptosis occurrence in a rat astrocyte cell line
No full textAIMS: The worldwide increase in aging population is prevalently associated with the increase of neurodegenerative diseases. Peroxisome Proliferator-Activated Receptors (PPARs) are ligand-modulated transcriptional factors which belong to the nuclear hormone receptor superfamily which regulates peroxisome proliferation. The PPAR-γ is the most extensively studied among the three isoforms and the neuroprotective effects of PPAR-γ agonists have been recently demonstrated in a variety of preclinical models of neurological disorders. The aim of the study is to biologically evaluate the neuroprotective effects of new PPAR-γ selective agonists in an in vitro model. MAIN METHODS: CTX-TNA2 rat astrocytes were treated with G3335, a PPAR-γ antagonist, to simulate the conditions of a neurological disorder. Newly synthetized PPAR-γ selective agonists were added to the cell culture. Cytotoxicity was assessed by MTT assay, catalase activity was investigated by a colorimetric assay, Reactive Oxygen Species (ROS) production and apoptosis occurrence were measured by flow cytometry. Western blotting were performed to measure the levels of protein involved in the apoptotic pathway. KEY FINDINGS: Four PPAR-γ agonists were selected. Among them, the GL516, a fibrate derivative, showed low cytotoxicity and proved effective in restoring the catalase activity, reducing ROS production and decreasing the apoptosis occurrence triggered by the G3335 administration. The effects of this molecule appear to be comparable to the reference compound rosiglitazone, a potent and selective PPAR-γ agonist, mainly at prolonged exposure times (96 h). SIGNIFICANCE: Based on recent evidence, hypofunctionality of the PPAR-γ in glial cells could be present in neurodegenerative diseases and could participate in pathological mechanisms through peroxisomal damage. The fibrate derivative PPAR-γ agonist GL516 emerged as the most promising molecule of the series and could have a role in preventing the pathophysiology of neurodegenerative disorders
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