16635-00-0Relevant articles and documents
Design, synthesis, and SAR analysis of novel selective σ1 ligands
Collina, Simona,Loddo, Guya,Urbano, Mariangela,Linati, Laura,Callegari, Athos,Ortuso, Francesco,Alcaro, Stefano,Laggner, Christian,Langer, Thierry,Prezzavento, Orazio,Ronsisvalle, Giuseppe,Azzolina, Ornella
, p. 771 - 783 (2007)
A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to σ1 and σ2 receptors. Many compounds exhibited nanomolar affinity for σ1 subtype receptor with good selectivity over σsub
Terminal-Selective Functionalization of Alkyl Chains by Regioconvergent Cross-Coupling
Dupuy, Stéphanie,Zhang, Ke-Feng,Goutierre, Anne-Sophie,Baudoin, Olivier
supporting information, p. 14793 - 14797 (2016/11/23)
Hydrocarbons are still the most important precursors of functionalized organic molecules, which has stirred interest in the discovery of new C?H bond functionalization methods. We describe herein a new step-economical approach that enables C?C bonds to be constructed at the terminal position of linear alkanes. First, we show that secondary alkyl bromides can undergo in situ conversion into alkyl zinc bromides and regioconvergent Negishi coupling with aryl or alkenyl triflates. The use of a suitable phosphine ligand favoring Pd migration enabled the selective formation of the linear cross-coupling product. Subsequently, mixtures of secondary alkyl bromides were prepared from linear alkanes by standard bromination, and regioconvergent cross-coupling then provided access to the corresponding linear arylation product in only two steps.
Identification of a potent and selective ρ1 receptor agonist potentiating NGF-induced neurite outgrowth in PC12 cells
Rossi, Daniela,Pedrali, Alice,Urbano, Mariangela,Gaggeri, Raffaella,Serra, Massimo,Fernández, Leyden,Fernández, Michael,Caballero, Julio,Ronsisvalle, Simone,Prezzavento, Orazio,Schepmann, Dirk,Wuensch, Bernhard,Peviani, Marco,Curti, Daniela,Azzolina, Ornella,Collina, Simona
scheme or table, p. 6210 - 6224 (2011/12/02)
Herein we report the synthesis, drug-likeness evaluation, and in vitro studies of new sigma (ρ) ligands based on arylalkenylaminic scaffold. For the most active olefin the corresponding arylalkylamine was studied. Novel arylalkenylamines generally possess