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Your search keyword '"Stasi, Luigi"' showing total 2 results
Start Over Author "Stasi, Luigi" Topic cytochrome p-450
2 results on '"Stasi, Luigi"'

1. Discovery, synthesis, selectivity modulation and DMPK characterization of 5-azaspiro[2.4]heptanes as potent orexin receptor antagonists.

Author

Stasi, Luigi Piero, Artusi, Roberto, Bovino, Clara, Buzzi, Benedetta, Canciani, Luca, Caselli, Gianfranco, Colace, Fabrizio, Garofalo, Paolo, Giambuzzi, Silvia, Larger, Patrice, Letari, Ornella, Mandelli, Stefano, Perugini, Lorenzo, Pucci, Sabrina, Salvi, Matteo, and Toro, PierLuigi

Subjects
*HEPTANE, *OREXINS, *SUBSTITUTION reactions, *PHARMACOKINETICS, *MATHEMATICAL optimization, *CYTOCHROME P-450, *DRUG development, *ORGANIC synthesis
Abstract

Abstract: Starting from a orexin 1 receptor selective antagonist 4,4-disubstituted piperidine series a novel potent 5-azaspiro[2.4]heptane dual orexin 1 and orexin 2 receptor antagonist class has been discovered. SAR and Pharmacokinetic optimization of this series is herein disclosed. Lead compound 15 exhibits potent activity against orexin 1 and orexin 2 receptors along with low cytochrome P450 inhibition potential, good brain penetration and oral bioavailability in rats. [Copyright &y& Elsevier]

Published
2013
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2. Synthesis, pharmacophore modeling and in vitro activity of 10,11-dihydrodibenzo[b,f]oxepine-4-carboxamide derivatives as novel and potent antagonists of the prostaglandin EP4 receptor

Author

Stasi, Luigi Piero, Bhimani, Kanji, Borriello, Manuela, Canciani, Luca, Caselli, Gianfranco, Colace, Fabrizio, Ferioli, Cristian, Kaswala, Mehul, Mennuni, Laura, Piepoli, Tiziana, Pucci, Sabrina, Salvi, Matteo, Shirsath, Vikas, Zanelli, Tiziano, and Zerbi, Silvia

Subjects
*PROSTAGLANDINS, *CYTOCHROME P-450, *PHARMACEUTICAL chemistry, *DRUG design, *DRUG derivatives, *PREDICTION models
Abstract

Abstract: The construction of a EP4 antagonists pharmacophore model and the discovery of a highly potent oxepinic series of EP4 antagonists is discussed. Compound 1a exhibits an excellent selectivity profile toward EP2 receptor subtype and low cytochrome P450 inhibition potential. [Copyright &y& Elsevier]

Published
2011
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