Výsledky vyhledávání - "Alfredo Cugola"

Synthesis of Substituted Indole-2-carboxylates: Versatile Introduction of a Carbamoyl Moiety at the C-3 Position

Autor: Simone Giacobbe, Davide Baraldi, Daniele Donati, Romano Di Fabio, Alfredo Cugola

Publikováno v: Synthetic Communications. 29:3125-3135

This paper deals with a novel and versatile synthetic approach for the introduction of a functionalized ethynyl side chain at the C-3 position of the 2-carboxyindole nucleus. The key step of this process is represented by the coupling reaction betwee

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b490df48d566dca9e939306dd86ad1fc
https://doi.org/10.1080/00397919908085936

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Cycloalkyl Indole-2-Carboxylates as Useful Tools for Mapping the 'North-Eastern' Region of the Glycine Binding Site Associated with the NMDA Receptor

Autor: Paola Gastaldi, Giovanni Gaviraghi, Alessandra Orlandi, Ornella Curcuruto, Aldo Feriani, Frank van Amsterdam, Carla Marchioro, Romano Di Fabio, Alfonso Pozzan, Alfredo Cugola, Anna M. Quaglia, Angelo Reggiani, Anna Maria Capelli, Fabrizio Micheli

Publikováno v: Archiv der Pharmazie. 332:73-80

A novel series of indole-2-carboxylate analogues of GV 150526 (1) in which the terminal phenyl ring belonging to the side chain present in the position C-3 has been replaced with a bridged cycloalkyl group was synthesized and evaluated for its pharma

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3c076e04e1996778cbf24501ad75fa4
https://doi.org/10.1002/(sici)1521-4184(19993)332:3<73::aid-ardp73>3.0.co

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New Synthesis of Substituted 2-Carboxyindole Derivatives: Versatile Introduction of a Carbamoylethynyl Moiety at the C-3 Position

Autor: Cheryl T. Hewkin, Alfredo Cugola, Paola Gastaldi, Romano Di Fabio, Nadia Conti, Fabrizio Micheli, Anna M. Quaglia

Publikováno v: Archiv der Pharmazie. 332:55-58

A novel series of 3-carbamoylethynyl-2-carboxyindoles, antagonists acting at the strychnine-insensitive glycine binding site associated with the NMDA receptor, has been synthesised. This new versatile approach involves the introduction of a 2-chloroe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38135c7ac174c992de0797c33fd59f70
https://doi.org/10.1002/(sici)1521-4184(19993)332:2<55::aid-ardp55>3.0.co

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2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide as selective glycine antagonist with in vivo activity

Autor: Giorgio Tarzia, Andrea Missio, Alfredo Cugola, Angelo Reggiani, Angelo Pecunioso, Fabrizio Micheli, Daniele Donati

Publikováno v: Bioorganic & Medicinal Chemistry. 5:2129-2132

2,3-Dihydro-6,7-dichloro-pyrido[2,3-b]pyrazine-8-oxide was synthesized and evaluated for in vitro/in vivo antagonistic activity at the strychnine insensitive glycine binding site on the NMDA receptor revealing it to be a useful tool to evaluate the e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f12ba2378d98d3f21d6371eab9acf70
https://doi.org/10.1016/s0968-0896(97)00156-9

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Substituted Indole-2-carboxylates as in Vivo Potent Antagonists Acting as the Strychnine-Insensitive Glycine Binding Site

Autor: Luciana Rossi, A. Feriani, Fabrizio Micheli, Anna M. Quaglia, Anna-Maria Capelli, David G. Trist, Paola Gastaldi, Angelo Reggiani, Alfredo Cugola, E. Ratti, Daniele Donati, Angelo Pecunioso, Manolo Mugnaini, Cheryl T. Hewkin, R. Di Fabio, Nadia Conti, Giovanna Tedesco, Andrea Missio, Giovanni Gaviraghi

Publikováno v: Journal of Medicinal Chemistry. 40:841-850

A series of indole-2-carboxylates bearing suitable chains at the C-3 position of the indole nucleus was synthesized and evaluated in terms of in vitro affinity using [3H]glycine binding assay and in vivo potency by inhibition of convulsions induced b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::27560a1551c483698a602ee0a0e903ed
https://doi.org/10.1021/jm960644a

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Synthesis and biological evaluation of pyrido[2,3-b]pyrazine and pyrido[2,3-b]pyrazine-n-oxide as selective glycine antagonists

Autor: Fabrizio Micheli, Giorgio Tarzia, M. Guarneri, Daniele Donati, Angelo Reggiani, Alfredo Cugola, Angelo Pecunioso, Andrea Missio, V. Zanirato

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:2749-2754

Pyrido[2,3-b]pyrazines and pyrido[2,3-b]purazines-N-oxides have been synthesized and evaluated for in vitro/in vivo antagonistic activity at the glycine site on the NMDA receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3deb7809726391fdf19db9f8b3d55c9d
https://doi.org/10.1016/s0960-894x(96)00492-1

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