104,762 research outputs found

    Novel bicyclic Delta2-isoxazoline and 3-oxo-isoxazolidine derivatives: synthesis and binding affinity at neuronal nicotinic receptor subtypes

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    Neuronal nicotinic acetylcholine receptors (nAChRs) are involved in various processes such as cognition, learning and memory, cerebral blood flow and metabolism, as well as an array of pathological conditions such as Alzheimer’s and Parkinson’s diseases, mild cognitive impairment (MCI), schizophrenia, epilepsy, Tourette’s syndrome, anxiety, depression, attention-deficit hyperactivity disorder (ADHD), and nicotine addiction. As an extension of our studies focused on new Delta2-isoxazoline derivatives and their affinity/efficacy profiles at alpha4beta2 and alpha7 nAChRs [1, 2], we synthesized the group of derivatives 4-9, which may be related to (-)-Cytisine 1 and (-)-Norferruginine 3. The target chiral compounds, obtained by means of pericyclic reactions, were prepared and tested as racemates. The synthetic details and the results of the pharmacological investigation will be presented and discussed. [1] Dallanoce, C.; Bazza, P.; Grazioso, G.; De Amici, M.; Gotti, C.; Riganti, L.; Clementi, F.; De Micheli, C. Synthesis of Epibatidine-related 2-Ixoxazoline Derivatives and Evaluation of their Binding Affinity at Neuronal Nicotinic Acetylcholine Receptors. Eur. J. Org. Chem. 2006; 3746-3754. [2] De Micheli, C.; De Amici, M.; Dallanoce, C.; Clementi, F.; Gotti, C. Preparation of Azabicyclic Spiro Compounds as Agonists of 7 Nicotinic Acetylcholine Receptors. PCT Int. Appl. WO 2008000469 (2008)

    In silico design of agonists targeting the alpha7 nicotinic acetylcholine receptors, their synthesis and preliminary pharmacological evaluation

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    As an extension of previous molecular modeling studies on nicotinic acetylcholine receptor (nAChR) ligands,[1] we now adopted the LIR (Linear Interaction Response) approach to reach a realistic compromise between accuracy and calculation rate, during the delta(G)bind value estimation of a training set of known agonists for the alpha7 nAChR subtype. The same strategy was applied to a text set of potential alpha7 nAChR agonists, which allowed identification of general structures A and B as the most promising ligands in the series. Thus, some of these derivatives were synthesized along with procedures previously utilized by us,[2] and were then assayed for binding affinity at alpha7 and alpha4beta2 nAChR subtypes. [1] Grazioso, G.; Cavalli, A.; De Amici, M.; Recanatini, M.; De Micheli, C. J. Comput. Chem. 2008, 29, 2593-2602. [2] Rizzi, L.; Dallanoce, C.; Matera, C.; Magrone, P.; Pucci, L.; Gotti, C.; Clementi, F.; De Amici, M. Bioorg. Med. Chem. Lett. 2008, 18, 4651-4654

    Globalizzazione e localizzazione nel discorso giuridico

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    Il volume raccoglie una serie di studi di linguisti e giuristi sulla comunicazione giuridica nel mondo contemporaneo, ponendosi in una prospettiva interdisciplinare grazie alla quale si combinano competenze diverse e ugualmente legittime su un comune oggetto di indagine

    La istoria di Eneas vulgarizata per Angilu di Capita, a cura di G. Folena. Collezione di testi siciliani... dir. da E. Li Gotti, 1956

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    Pézard André. La istoria di Eneas vulgarizata per Angilu di Capita, a cura di G. Folena. Collezione di testi siciliani... dir. da E. Li Gotti, 1956. In: Romania, tome 81 n°321, 1960. pp. 126-128

    La istoria di Eneas vulgarizata per Angilu di Capita, a cura di G. Folena. Collezione di testi siciliani... dir. da E. Li Gotti, 1956

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    Pézard André. La istoria di Eneas vulgarizata per Angilu di Capita, a cura di G. Folena. Collezione di testi siciliani... dir. da E. Li Gotti, 1956. In: Romania, tome 81 n°321, 1960. pp. 126-128
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