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Your search keyword '"Carullo, Gabriele"' showing total 5 results
Start Over Author "Carullo, Gabriele" Journal european journal of medicinal chemistry
5 results on '"Carullo, Gabriele"'

1. Development of potent and selective FAAH inhibitors with improved drug-like properties as potential tools to treat neuroinflammatory conditions

Author

Papa, Alessandro, Pasquini, Silvia, Galvani, Francesca, Cammarota, Mariarosaria, Contri, Chiara, Carullo, Gabriele, Gemma, Sandra, Ramunno, Anna, Lamponi, Stefania, Gorelli, Beatrice, Saponara, Simona, Varani, Katia, Mor, Marco, Campiani, Giuseppe, Boscia, Francesca, Vincenzi, Fabrizio, Lodola, Alessio, and Butini, Stefania

Published
2023
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2. Azetidin-2-one-based small molecules as dual hHDAC6/HDAC8 inhibitors: Investigation of their mechanism of action and impact of dual inhibition profile on cell viability

Author

Federico, Stefano, Khan, Tuhina, Fontana, Anna, Brogi, Simone, Benedetti, Rosaria, Sarno, Federica, Carullo, Gabriele, Pezzotta, Alex, Saraswati, Akella Prasanth, Passaro, Eugenia, Pozzetti, Luca, Papa, Alessandro, Relitti, Nicola, Gemma, Sandra, Butini, Stefania, Pistocchi, Anna, Ramunno, Anna, Vincenzi, Fabrizio, Varani, Katia, Tatangelo, Vanessa, Patrussi, Laura, Baldari, Cosima T., Saponara, Simona, Gorelli, Beatrice, Lamponi, Stefania, Valoti, Massimo, Saccoccia, Fulvio, Giannaccari, Marialaura, Ruberti, Giovina, Herp, Daniel, Jung, Manfred, Altucci, Lucia, and Campiani, Giuseppe

Published
2022
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3. Design and synthesis of multifunctional microtubule targeting agents endowed with dual pro-apoptotic and anti-autophagic efficacy

Author

Campiani, Giuseppe, Khan, Tuhina, Ulivieri, Cristina, Staiano, Leopoldo, Papulino, Chiara, Magnano, Stefania, Nathwani, Seema, Ramunno, Anna, Lucena-Agell, Daniel, Relitti, Nicola, Federico, Stefano, Pozzetti, Luca, Carullo, Gabriele, Casagni, Alice, Brogi, Simone, Vanni, Francesca, Galatello, Paola, Ghanim, Magda, McCabe, Niamh, Lamponi, Stefania, Valoti, Massimo, Ibrahim, Ola, O'Sullivan, Jeffrey, Turkington, Richard, Kelly, Vincent P., VanWemmel, Ruben, Díaz, J. Fernando, Gemma, Sandra, Zisterer, Daniela, Altucci, Lucia, De Matteis, Maria Antonietta, Butini, Stefania, and Benedetti, Rosaria

Published
2022
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5. Development of potent and selective FAAH inhibitors with improved drug-like properties as potential tools to treat neuroinflammatory conditions

Author

Alessandro Papa, Silvia Pasquini, Francesca Galvani, Mariarosaria Cammarota, Chiara Contri, Gabriele Carullo, Sandra Gemma, Anna Ramunno, Stefania Lamponi, Beatrice Gorelli, Simona Saponara, Katia Varani, Marco Mor, Giuseppe Campiani, Francesca Boscia, Fabrizio Vincenzi, Alessio Lodola, Stefania Butini, Papa, Alessandro, Pasquini, Silvia, Galvani, Francesca, Cammarota, Mariarosaria, Contri, Chiara, Carullo, Gabriele, Gemma, Sandra, Ramunno, Anna, Lamponi, Stefania, Gorelli, Beatrice, Saponara, Simona, Varani, Katia, Mor, Marco, Campiani, Giuseppe, Boscia, Francesca, Vincenzi, Fabrizio, Lodola, Alessio, and Butini, Stefania

Subjects
Pharmacology, Endocannabinoid system, Enzyme inhibitors, Fatty acid amide hydrolase, Neuroinflammation, Neuroprotection, Reversible inhibitors, Selective inhibitors, Reversible inhibitor, Organic Chemistry, Enzyme inhibitor, General Medicine, Drug Discovery
Abstract

The neuroprotective performance against neuroinflammation of the endocannabinoid system (ECS) can be remarkably improved by indirect stimulation mediated by the pharmacological inhibition of the key ECS catabolic enzyme fatty acid amide hydrolase (FAAH). Based on our previous works and aiming to discover new selective FAAH inhibitors , we herein reported a new series of carbamate-based FAAH inhibitors (4a-t) which showed improved drug disposition properties compared to the previously reported analogues 2a-b. The introduction of ionizable functions allowed us to obtain new FAAH inhibitors of nanomolar potency characterized by good water solubility and chemical stability at physiological pH. Interesting structure-activity relationships (SARs), deeply analyzed by molecular docking and molecular dynamic (MD) simulations, were obtained. All the newly developed inhibitors showed an excellent selectivity profile evaluated against monoacylglycerol lipase and cannabinoid receptors. The reversible mechanism of action was determined by a rapid dilution assay. Absence of toxicity was confirmed in mouse fibroblasts NIH3T3 (for compounds 4e, 4g, 4n-o, and 4s) and in human astrocytes cell line 1321N1 (for compounds 4e, 4n, and 4s). The absence of undesired cardiac effects was also confirmed for compound 4n. Selected analogues (compounds 4e, 4g, 4n, and 4s) were able to reduce oxidative stress in 1321N1 astrocytes and exhibited notable neuroprotective effects when tested in an ex vivo model of neuroinflammation.

Published
2022

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