Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Angelica Mazzali"'
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
Autor:
Ceri H. Davies, Adrianna Teriakidis, Anita K. Roopun, James N.C. Kew, Andrew D. Randall, Zining Wu, Hugh J. Herdon, Jon T. Brown, Ross Jeggo, Nisha Patel, Ian Thomson Forbes, Clive Leslie Branch, Gareth A. Jones, Miles A. Whittington, Victoria Anne Honey Fry, Nigel E. Austin, Martyn D. Wood, Rosemary A. Melarange, Katherine A. Buchanan, Joanne Pardoe, Christopher J. Langmead, Claire Roberts, Kathryn R. Starr, Angelica Mazzali, Jeannette M. Watson, Jim J. Hagan
Publikováno v:
British Journal of Pharmacology. 154:1104-1115
Background and purpose: M1 muscarinic ACh receptors (mAChRs) represent an attractive drug target for the treatment of cognitive deficits associated with diseases such as Alzheimer's disease and schizophrenia. However, the discovery of subtype-selecti
Autor:
Marinella Roberti, Natale D'Alessandro, Angelica Mazzali, Riccardo Rondanin, Manlio Tolomeo, Daniele Simoni, Marcello Rossi, Luisa Dusonchet, Cinzia Malagutti, Maria Meli, Riccardo Baruchello, Francesco Paolo Invidiata, Stefania Grimaudo, Maria Valeria Raimondi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2669-2673
Considering that the stereochemistry of the C9-C10 alkenyl portion of natural 9-cis-RA, as the one of the olefinic moiety of the previously described isoxazole retinoid 4, seems of particular importance for their apoptotic activity, we prepared a nov
Autor:
Francesco Paolo Invidiata, Marinella Roberti, Daniele Simoni, Riccardo Rondanin, Riccardo Baruchello, Cinzia Malagutti, Marcello Rossi, Angelica Mazzali
Publikováno v:
Organic Letters. 2:3765-3768
A convenient procedure to effect the Wittig and Horner-Wadsworth-Emmons reactions employs guanidine TBD and MTBD as base-promoters; mild reaction conditions, high efficiency, and facile isolation of the final products make the present methodology, at
Autor:
Colin Philip Leslie, Laura Zonzini, Stefania Contini, Domenica Antonia Pizzi, Angelica Mazzali, Jonathan Mark Bentley, Matteo Biagetti, Romano Di Fabio, Fabio Maria Sabbatini, Laura Caberlotto, Catia Seri, Thorsten Genski
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(23)
A novel class of benzimidazole NPY Y5 receptor antagonists was prepared exploiting a privileged spirocarbamate moiety. The structure-activity relationship of this series and efforts to achieve a profile suitable for further development and an appropr
Autor:
Dhar Arindam, Shennan Lu, Marinella Roberti, Maria Valeria Raimondi, Luisa Dusonchet, Stefania Grimaudo, Marcello Rossi, Natale D'Alessandro, Daniele Simoni, Cinzia Malagutti, Angelica Mazzali, Marilena Landino, Riccardo Rondanin, Riccardo Baruchello, Maria Meli, Manlio Tolomeo, Francesca Capone, Doris M. Benbrook, Francesco Paolo Invidiata
Publikováno v:
Journal of medicinal chemistry. 44(14)
In a search for retinoic acid (RA) receptor ligands endowed with potent apoptotic activity, a series of novel arotinoids were prepared. Because the stereochemistry of the C9-alkenyl portion of natural 9-cis-RA and the olefinic moiety of the previousl
Autor:
Francesco Paolo Invidiata, Marcello Rossi, Marinella Roberti, Riccardo Rondanin, Daniele Simoni, Cinzia Malagutti, Riccardo Baruchello, Angelica Mazzali
Publikováno v:
ChemInform. 32
A convenient procedure to effect the Wittig and Horner−Wadsworth−Emmons reactions employs guanidine TBD and MTBD as base-promoters; mild reaction conditions, high efficiency, and facile isolation of the final products make the present methodology