Elisa Magli, Caterina Fattorusso, Marco Persico, Angela Corvino, Gianluca Esposito, Ferdinando Fiorino, Paolo Luciano, Elisa Perissutti, Vincenzo Santagada, Beatrice Severino, Valentina Tedeschi, Anna Pannaccione, Giuseppe Pignataro, Giuseppe Caliendo, Lucio Annunziato, Agnese Secondo, Francesco Frecentese
Due to the neuroprotective role of the Na+ /Ca2+ exchanger (NCX) isoforms NCX1 and NCX3, we synthesized novel benzodiazepinone derivatives of the unique NCX activator Neurounina-1 , named compounds 1-19 . The derivatives are characterized by a benzodiazepinonic nucleus linked to five- or six-membered cyclic amines via a methylene, ethylene, or acetyl spacer. The compounds have been screened on NCX1/NCX3 isoform activities by a high-throughput screening approach, and the most promising were characterized by patch-clamp electrophysiology and Fura-2AM video imaging...
November 30, 2021: Journal of Medicinal Chemistry