Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Laura Zonzini"'
Autor:
Aldo Feriani, Laura Zonzini, Laura Castelletti, Selena Nola, Michele Dal Cin, Teresa Semeraro, Sylvie Gehanne, Silvia Tomelleri, Filippo Visentini, Palmina Cavallini, Susanna Cremonesi, Annalisa Pellacani, Anna Sava, Alessia Bacchi, Andrea Wong, Simone Braggio, Luca Tarsi, Mahmud Kajbaf, Paolo Cavanni, Elisabetta Perdona, Christian Heidbreder, Luciano Marchiò, Beatrice Oliosi, Fabrizio Micheli
Publikováno v:
Journal of Medicinal Chemistry. 59:8549-8576
A novel series of 1,2,4-triazolyl 5-azaspiro[2.4]heptanes with high affinity and selectivity at the dopamine (DA) D3 receptor (D3R) is described. Some of these compounds also have high selectivity over the hERG channel and were characterized with res
Autor:
Michele Dal Cin, Susanna Cremonesi, Simone Braggio, Andrea Wong, Aldo Feriani, Laura Zonzini, Andrea Bernardelli, Laura Castelletti, Federica Bianchi, Filippo Visentini, Palmina Cavallini, Teresa Semeraro, Silvia Tomelleri, Luca Tarsi, Christian Heidbreder, Paolo Cavanni, Fabrizio Micheli, Beatrice Oliosi
Publikováno v:
Bioorganicmedicinal chemistry. 24(8)
A novel series of 1,2,4-triazolyl octahydropyrrolo[2,3-b]pyrroles showing high affinity and selectivity at the DA D3 receptor is reported here. Compounds endowed with high selectivity over the hERG channel were identified and their pharmacokinetic pr
Autor:
Romano Di Fabio, Emiliangelo Ratti, Sergio Melotto, Mauro Corsi, Laura Zonzini, Giuseppe Alvaro, Daniele Donati, Cristiana Griffante, Domenica Antonia Pizzi, Zadeo Cimarosti, Stefano Provera, Philip Gerrard, David G. Trist, Giuseppe Guercio, Carla Marchioro, Dino Montanari, Mario Mattioli
Publikováno v:
Journal of Medicinal Chemistry. 54:1071-1079
A large body of compelling preclinical evidence supports the clinical use of neurokinin (NK) receptor antagonists in a plethora of CNS and non-CNS therapeutic areas. The significant investment made in this area over the past 2 decades culminated with
Autor:
Laurie J. Gordon, Anna-Maria Capelli, Laura Zonzini, Manuela Borriello, Romano Di-Fabio, Enrica Granci, Massimo Gianotti, Roberto Arban, Simone Spada, Barbara Bertani, Stefania Faedo, Valeria Zucchelli, Alessandra Pasquarello, Angela Worby, Steven Mark Bromidge
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7092-7096
5-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones have been identified with different combinations of 5-HT(1) autoreceptor antagonist and hSerT potencies and excellent rat PK profiles. The avai
Discovery and structure–activity relationship of a novel spirocarbamate series of NPY Y5 antagonists
Autor:
Jonathan Mark Bentley, Matteo Biagetti, Laura Caberlotto, Colin Philip Leslie, Romano Di Fabio, Thorsten Genski, Daniele Donati, Laura Zonzini, Catia Seri, Sebastien Guery, Stefania Contini, Angelica Mazzali, Domenica Antonia Pizzi, Michela Tessari, Giancarlo Merlo, Fabiola Sacco
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6103-6107
A novel series of trans-8-aminomethyl-1-oxa-3-azaspiro[4.5]decan-2-one derivatives was identified with potent NPY Y5 antagonist activity. Optimization of the original lead furnished compounds 23p and 23u, which combine sub-nanomolar Y5 activity with
Autor:
Laura Caberlotto, Thorsten Genski, Matteo Biagetti, Domenica Antonia Pizzi, Colin Philip Leslie, Laura Zonzini, Jonathan Mark Bentley, Angelica Mazzali, Catia Seri, Romano Di Fabio
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4741-4744
A novel class of small molecule NPY Y5 antagonists based around an azabicyclo[3.1.0]hexane scaffold was identified through modification of a screening hit. Structure–activity relationships and efforts undertaken to achieve a favourable pharmacokine
Publikováno v:
Expert Opinion on Drug Discovery. 5:1031-1037
The importance of evaluating drug metabolism and pharmacokinetic (DMPK) properties very early in the drug discovery process in order to reduce attrition during development is now well recognised. In this paper we illustrate an approach for PK screeni
Autor:
Ilaria Sartori, Laura Zonzini, Laurie J. Gordon, Angela Worby, Stefano Fontana, Manuela Borriello, Silvia Bison, Jeannette M. Watson, Steven Mark Bromidge, Giovanna Dal Forno, Colin Philip Leslie, Alessandra Pasquarello, Anna Sava, Luca G. Moccia, Barbara Bertani, Roberto Arban, Daniele Donati, Enrica Granci, Valeria Zucchelli, Paolo Cavanni, Massimo Gianotti, Romano Di-Fabio
Publikováno v:
Journal of Medicinal Chemistry. 53:5827-5843
Bioisoteric replacement of the metabolically labile N-methyl amide group of a series of benzoxazinones with small heterocyclic rings has led to novel series of fused tricyclic benzoxazines which are potent 5-HT1A/B/D receptor antagonists with and wit
Autor:
Romano Di Fabio, Giovanna Tedesco, Laura Zonzini, Gunther Scheid, Fabrizio Micheli, Ornella Perini, Beatrice Oliosi, Michela Bettati, Paolo Cavanni
Publikováno v:
ChemMedChem. 5:361-366
Autor:
Laura Zonzini, Giuseppe Alvaro, Stefano Provera, Giorgio Pentassuglia, Daniele Donati, Cristiana Griffante, Zadeo Cimarosti, Giuseppe Guercio, Carla Marchioro, Romano Di Fabio, Mario Mattioli, David G. Trist, Dino Montanari, Mauro Corsi, Philip Gerrard, Domenica Antonia Pizzi, Emiliangelo Ratti, Tino Rossi, Sergio Melotto
Publikováno v:
Journal of Medicinal Chemistry. 52:3238-3247
In an effort to discover novel druglike NK1 receptor antagonists a new series of suitably substituted C-phenylpiperazine derivatives was identified by an appropriate chemical exploration of related N-phenylpiperazine analogues, with the specific aim