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Start Over Author "Pannaccione, Anna" Journal journal of medicinal chemistry
7 results on '"Pannaccione, Anna"'

2. New Insights into the Structure–Activity Relationship and Neuroprotective Profile of Benzodiazepinone Derivatives of Neurounina-1 as Modulators of the Na+/Ca2+ Exchanger Isoforms

Author

Magli, Elisa, primary, Fattorusso, Caterina, additional, Persico, Marco, additional, Corvino, Angela, additional, Esposito, Gianluca, additional, Fiorino, Ferdinando, additional, Luciano, Paolo, additional, Perissutti, Elisa, additional, Santagada, Vincenzo, additional, Severino, Beatrice, additional, Tedeschi, Valentina, additional, Pannaccione, Anna, additional, Pignataro, Giuseppe, additional, Caliendo, Giuseppe, additional, Annunziato, Lucio, additional, Secondo, Agnese, additional, and Frecentese, Francesco, additional

Published
2021
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3. Synthesis and Characterization of Novel Mono- and Bis-Guanyl Hydrazones as Potent and Selective ASIC1 Inhibitors Able to Reduce Brain Ischemic Insult

Author

Gornati, Davide, primary, Ciccone, Roselia, additional, Vinciguerra, Antonio, additional, Ippati, Stefania, additional, Pannaccione, Anna, additional, Petrozziello, Tiziana, additional, Pizzi, Erika, additional, Hassan, Amal, additional, Colombo, Eleonora, additional, Barbini, Stefano, additional, Milani, Mario, additional, Caccavone, Cecilia, additional, Randazzo, Pietro, additional, Muzio, Luca, additional, Annunziato, Lucio, additional, Menegon, Andrea, additional, Secondo, Agnese, additional, Mastrangelo, Eloise, additional, Pignataro, Giuseppe, additional, and Seneci, Pierfausto, additional

Published
2021
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4. New Insights into the Structure-Activity Relationship and Neuroprotective Profile of Benzodiazepinone Derivatives of Neurounina-1 as Modulators of the Na+/Ca2+ Exchanger Isoforms.

Author

Magli, Elisa, Fattorusso, Caterina, Persico, Marco, Corvino, Angela, Esposito, Gianluca, Fiorino, Ferdinando, Luciano, Paolo, Perissutti, Elisa, Santagada, Vincenzo, Severino, Beatrice, Tedeschi, Valentina, Pannaccione, Anna, Pignataro, Giuseppe, Caliendo, Giuseppe, Annunziato, Lucio, Secondo, Agnese, and Frecentese, Francesco

Published
2021
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5. New Insights into the Structure–Activity Relationship and Neuroprotective Profile of Benzodiazepinone Derivatives of Neurounina-1as Modulators of the Na+/Ca2+Exchanger Isoforms

Author

Magli, Elisa, Fattorusso, Caterina, Persico, Marco, Corvino, Angela, Esposito, Gianluca, Fiorino, Ferdinando, Luciano, Paolo, Perissutti, Elisa, Santagada, Vincenzo, Severino, Beatrice, Tedeschi, Valentina, Pannaccione, Anna, Pignataro, Giuseppe, Caliendo, Giuseppe, Annunziato, Lucio, Secondo, Agnese, and Frecentese, Francesco

Abstract

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. We identified two novel modulators of NCX: compound 4, inhibiting NCX1 reverse mode, and compound 14, enhancing NCX1 and NCX3 activity. Compound 1displayed neuroprotection in two preclinical models of brain ischemia. The analysis of the conformational and steric features led to the identification of the molecular volume required for selective NCX1 activation for mixed NCX1/NCX3 activation or for NCX1 inhibition, providing the first prototypal model for the design of optimized isoform modulators.

Published
2021
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6. New Insights into the Structure–Activity Relationship and Neuroprotective Profile of Benzodiazepinone Derivatives of Neurounina-1 as Modulators of the Na+/Ca2+ Exchanger Isoforms

Author

Lucio Annunziato, Elisa Perissutti, Giuseppe Pignataro, Paolo Luciano, Agnese Secondo, Valentina Tedeschi, Giuseppe Caliendo, Caterina Fattorusso, Vincenzo Santagada, Angela Corvino, Elisa Magli, Anna Pannaccione, Francesco Frecentese, Beatrice Severino, Ferdinando Fiorino, Marco Persico, Gianluca Esposito, Magli, E., Fattorusso, C., Persico, M., Corvino, A., Esposito, G., Fiorino, F., Luciano, P., Perissutti, E., Santagada, V., Severino, B., Tedeschi, V., Pannaccione, Anna, Pignataro, G., Caliendo, G., Annunziato, L., Secondo, A., and Frecentese, F.

Subjects
Steric effects, Gene isoform, Benzodiazepinones, Ethylene, Pyrrolidines, Activator (genetics), Stereochemistry, Neuroprotection, Article, Sodium-Calcium Exchanger, chemistry.chemical_compound, Structure-Activity Relationship, medicine.anatomical_structure, Neuroprotective Agents, chemistry, Drug Design, Drug Discovery, medicine, cardiovascular system, Molecular Medicine, Structure–activity relationship, Animals, Protein Isoforms, Methylene, Nucleus
Abstract

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. We identified two novel modulators of NCX: compound 4, inhibiting NCX1 reverse mode, and compound 14, enhancing NCX1 and NCX3 activity. Compound 1 displayed neuroprotection in two preclinical models of brain ischemia. The analysis of the conformational and steric features led to the identification of the molecular volume required for selective NCX1 activation for mixed NCX1/NCX3 activation or for NCX1 inhibition, providing the first prototypal model for the design of optimized isoform modulators.

Published
2021

7. New Insights into the Structure-Activity Relationship and Neuroprotective Profile of Benzodiazepinone Derivatives of Neurounina-1 as Modulators of the Na + /Ca 2+ Exchanger Isoforms.

Author

Magli E, Fattorusso C, Persico M, Corvino A, Esposito G, Fiorino F, Luciano P, Perissutti E, Santagada V, Severino B, Tedeschi V, Pannaccione A, Pignataro G, Caliendo G, Annunziato L, Secondo A, and Frecentese F

Subjects
Animals, Benzodiazepinones chemistry, Drug Design, Protein Isoforms metabolism, Sodium-Calcium Exchanger metabolism, Structure-Activity Relationship, Benzodiazepinones pharmacology, Neuroprotective Agents pharmacology, Protein Isoforms antagonists & inhibitors, Pyrrolidines chemistry, Sodium-Calcium Exchanger antagonists & inhibitors
Abstract

Due to the neuroprotective role of the Na + /Ca 2+ 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. We identified two novel modulators of NCX: compound 4 , inhibiting NCX1 reverse mode, and compound 14 , enhancing NCX1 and NCX3 activity. Compound 1 displayed neuroprotection in two preclinical models of brain ischemia. The analysis of the conformational and steric features led to the identification of the molecular volume required for selective NCX1 activation for mixed NCX1/NCX3 activation or for NCX1 inhibition, providing the first prototypal model for the design of optimized isoform modulators.

Published
2021
Full Text
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