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

1. Novel analgesic/anti-inflammatory agents: 1,5-Diarylpyrrole nitrooxyethyl sulfides and related compounds as Cyclooxygenase-2 inhibitors containing a nitric oxide donor moiety endowed with vasorelaxant properties

Author

Saletti, Mario, Maramai, Samuele, Reale, Annalisa, Paolino, Marco, Brogi, Simone, Di Capua, Angela, Cappelli, Andrea, Giorgi, Gianluca, D'Avino, Danilo, Rossi, Antonietta, Ghelardini, Carla, Di Cesare Mannelli, Lorenzo, Sardella, Roccaldo, Carotti, Andrea, Woelkart, Gerald, Klösch, Burkhard, Bigogno, Chiara, Dondio, Giulio, and Anzini, Maurizio

Published
2022
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5. Synthesis and structure–activity relationship studies in serotonin 5-HT4 receptor ligands based on a benzo[de][2,6]naphthridine scaffold.

Author

Castriconi, Federica, Paolino, Marco, Giuliani, Germano, Anzini, Maurizio, Campiani, Giuseppe, Mennuni, Laura, Sabatini, Chiara, Lanza, Marco, Caselli, Gianfranco, De Rienzo, Francesca, Menziani, Maria Cristina, Sbraccia, Maria, Molinari, Paola, Costa, Tommaso, and Cappelli, Andrea

Subjects
*SEROTONIN receptors, *AMINOPYRIDINES, *LIGANDS (Biochemistry), *STRUCTURE-activity relationships, *CHEMICAL synthesis, *G protein coupled receptors, *GREEN fluorescent protein
Abstract

Abstract: A small series of serotonin 5-HT4 receptor ligands has been designed from flexible 2-methoxyquinoline compounds 7a,b by applying the conformational constraint approach. Ligands 7a,b and the corresponding conformationally constrained analogues 8a–g were synthesized and their interactions with the 5-HT4 receptor were examined by measuring both binding affinity and the ability to promote or inhibit receptor–G protein coupling. Ester derivative 7a and conformationally constrained compound 8b were demonstrated to be the most interesting compounds showing a nanomolar 5-HT4R affinity similar to that shown by reference ligands cisapride (1) and RS-23,597-190 (4). The result was rationalized by docking studies in term of high similarity in the binding modalities of flexible 7a and conformationally constrained 8b. The intrinsic efficacy of some selected ligands was determined by evaluating the receptor–G protein coupling and the results obtained demonstrated that the nature and the position of substituents play a critical role in the interaction of these ligands with their receptor. [Copyright &y& Elsevier]

Published
2014
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