1,721,011 research outputs found
Chiral Supramolecular Chemistry of Basket Resorc[4]arenes
Full text linkChiral Basket Resorc[4]arenes are well known chiral solvating agents that can induce enantiodiscrimination towards aminoacids, peptides and nucleosides. We synthesized both enantiomer of some basket resorc[4]arenes capable of forming stable diasteromeric host-guest complexes with some nucleosides like cytidine and cytarabine. The reactivity and the structures of the complexes were investigated in gas-phase (ESI-IRMPD, ESI-FT-ICR) and in solution (DOSY, ROESY). Different "in" and "out" structures were found both in solution and in gas-phase, moreover the results were supported by theoretical calculations
Phenolic compounds as likely natural mediators of laccase: A mechanistic assessment
No full textThe oxidation mechanism of non-phenolic substrates induced by laccase under catalysis by two phenolic mediators is shown to be radical. (C) 2007 Elsevier B.V. All rights reserved
The market of chiral drugs: chiral switches versus de novo enantiomerically pure compounds
No full textThis review article is aimed at providing an overview of the current market of chiral drugs by exploring which is the nowadays tendency, for the pharmaceutical industry, either to exploit the chiral switching practice from already marketed racemates or to develop de novo enantiomerically pure compounds. A concise illustration of the main techniques developed to assess the absolute configuration (AC) and enantiomeric purity of chiral drugs has been given, where greater emphasis was placed on the contribution of enantioselective chromatography (HPLC, SFC and UHPC).
Afterwards, we focused our study on the cohort of 45 new drugs that have been approved by the US Food and Drug Administration (FDA) in 2015. We extracted the chemical structure of the new drugs from the FDA approval chemistry reviews available on the database of the agency’s Center for Drug Evaluation and Research (CDER), and we selected a subgroup (i.e., 44% of the cohort) of small-molecule active pharmaceutical ingredients (APIs) containing one or more chirality centers
Profili di funzionamento cognitivo e difficoltà di apprendimento: analisi di cluster clinici della WISC-IV
No full textIl lavoro analizza i profili di funzionamento cognitivo ottenuti con la scala WISC-IV (Wechsler Intelligence Scale for Children, 2012) su gruppi di partecipanti con diagnosi differenziale formulata secondo i criteri definiti dalla Consensus Conference sui DSA (2010) e secondo le classificazioni ICD-10. I soggetti (112, di età compresa tra i 6 e i 16 anni) evidenziano tutti difficoltà d‘apprendimento, da riferirsi a differenti quadri diagnostici. Lo scopo principale dello studio è quello di analizzare la distribuzione dei punteggi ai principali indici sintetici della suddetta scala (IAG e ICC, oltre agli indici ICV, IRP, IML e IVE) e l‘ampiezza delle differenze tra gli indici stessi
B.E.S.CO.Batteria per l'esame delle strategie cognitive, a cura del Servizio di Psicologia dell'Apprendimento e dell'Educazione in Età Evolutiva
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Palladium-Catalyzed Synthesis of 6-aryl Dopamine Derivatives
Full text linkDopamine is a key neurotransmitter involved in a series of biologically relevant processes and its derivatives have sparked significant interest as intriguing synthetic targets. This class of compounds is indeed not only considerable for the potential biological activities but is also promising for diverse applications in material science. In light of this, our research was focused on the synthesis of 6-aryldopamine derivatives starting from 4-(2-aminoethyl)phenol through a sequential protocol, whose main steps are hydroxylation, halogenation, and Suzuki cross-coupling. Our method demonstrated versatility, efficiency, and compatibility with various functional groups, including aldehydes, ketones, esters, ethers, and fluorine
One hundred faces of cyclopamine
No full textThe natural steroidal alkaloid cyclopamine has been identified as the first inhibitor of the Hedgehog (Hh) signaling pathway, which is implicated in embryonic development and tumorigenesis, as well as is hyperactivated in cancer stem cells (CSCs). The list of Hh-dependent tumors is steadily growing, and it has been estimated that about 25% of all cancer deaths show signs of aberrant Hh pathway activation. Notably, cyclopamine has been found to exert anticancer activity against several types of human cancer and to inhibit CSCs proliferation, thus highlighting the druggability of the Hh pathway and paving new opportunities in anticancer drug discovery. The aim of the present work is to review the main synthetic strategies to cyclopamine and its derivatives, with particular emphasis on the challenging chemical modifications aimed at improving the biological activity of the molecule
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
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