Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Colin Philip Leslie"'
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:
Colin Philip Leslie, Massimo Gianotti, Corrado Corti, Laura Piccoli, Romano Di Fabio, Mark Wigglesworth, Luigi Piero Stasi, Sonia Delle Fratte, Francesca Pavone
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5069-5073
A novel imidazobenzazepine template (5a) with potent dual H1/5-HT2A antagonist activity was identified. Application of a zwitterionic approach to this poorly selective and poorly developable starting point successfully delivered a class of high quali
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:
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:
Daniele Donati, Francesca Pavone, Luigi Piero Stasi, Damiano Ghirlanda, Giorgio Pentassuglia, Riccardo Giovannini, Domenica Antonia Pizzi, Romano Di Fabio, Angelo Pecunioso, Colin Philip Leslie, Giovanna Dal Forno, Alessandro Falchi, Manuela Borriello, Francesca Bonetti, Giovanna Rumboldt, Simone Braggio
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1043-1046
The synthesis of a series of carbazole derivatives and their SAR at the NPY Y1 receptor is described. Modulation of physicochemical properties by appropriate decoration led to the identification of a high-affinity NPY Y1 antagonist that shows high br
Autor:
Francesco Nicotra, Francesco Peri, Colin Philip Leslie, Carla Marchioro, Fabrizio Micheli, Pierfausto Seneci
Publikováno v:
Journal of Carbohydrate Chemistry. 22:57-71
d‐Glucose derivatives bearing an anomeric thiophenyl group and orthogonally protections on secondary hydroxyl groups were linked to solid supports (PS/DV polymer, tentagel resin) through an ester bond on C‐6. It was investigated the possibility t
Autor:
Andrew J. P. White, Colin Philip Leslie, Jean-François Basset, Dieter Hamprecht, Anthony G. M. Barrett
Publikováno v:
Tetrahedron Letters. 51:783-785
6-(2,4-Dioxopentyl)-2,2-trimethyl-4H-1,3-dioxin-4-one on reflux in toluene gave MeCOCH2COCH2COCH C O, which cyclized to 6-(2-oxopropyl)-4-hydroxy-2H-pyran-2-one or was trapped with alcohols to produce resorcylate esters. The method was used for the s
Autor:
Romano Di Fabio, Massimo Gianotti, Colin Philip Leslie, Luigi Piero Stasi, Sonia Delle Fratte, Laura Piccoli, Mark Wigglesworth, Francesca Pavone, Corrado Corti
Publikováno v:
ChemInform. 42
The derivatives (I) are shown to possess potent and balanced H1/5-HT2A receptor antagonist activities.
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:
Catia Seri, Elisabetta Greco, Romano Di Fabio, Domenica Antonia Pizzi, Michele Negri, Alessandro Falchi, Colin Philip Leslie, Gennaro Carnevale, Laura Mangiarini, Giovanni Bernasconi, Michela Squaglia
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(1)
Two complementary stereospecific synthetic approaches for the preparation of unsymmetrical ortho-substituted N-(4,4-diphenylbut-3-enyl) derivatives of nipecotic acid are described. Determination of the activity of the prepared compounds at the GAT-1