Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Sergio A. Alonso De Diego"'
Autor:
Sergio A. Alonso de Diego, Daniel Oehlrich, Harrie J.M. Gijsen, Andrés A. Trabanco, Hana Prokopcová, Nigel Austin, Michel Surkyn, Dries Van den Bossche, Frederik J. R. Rombouts, Deborah Dhuyvetter, Gregor James Macdonald, Sven Franciscus Anna Van Brandt, Herman Borghys, Michiel Van Gool, Diederik Moechars, Aránzazu García-Molina, Michel Anna Jozef De Cleyn, Carolina Martinez-Lamenca
Publikováno v:
Journal of Medicinal Chemistry. 61:5292-5303
In previous studies, the introduction of electron withdrawing groups to 1,4-oxazine BACE1 inhibitors reduced the pKa of the amidine group, resulting in compound 2 that showed excellent in vivo efficacy, lowering Aβ levels in brain and CSF. However,
Autor:
Marijke Somers, Gregor James Macdonald, Oscar Delgado, Fabrice Jourdan, Sergio A. Alonso de Diego, Michiel Van Gool, Andrés A. Trabanco, Luc Ver Donck
Publikováno v:
ChemMedChem. 12:905-912
The metabotropic glutamate subtype 2 (mGlu2 ) receptor is a presynaptic membrane receptor distributed widely in brain that provides feedback inhibitory control of glutamate release. Inhibition of the mGlu2 receptor function with a negative allosteric
Autor:
Sven Franciscus Anna Van Brandt, Aldo Peschiulli, Andrés A. Trabanco, Ann Vos, Nigel Austin, Sergio A. Alonso de Diego, Michel Anna Jozef De Cleyn, Hana Prokopcová, Michel Surkyn, Dieder Moechars, Daniel Oehlrich, Gregor James Macdonald, Frederik J. R. Rombouts, Juan Antonio Vega, Michiel Van Gool, Ana Isabel de Lucas, Harrie J.M. Gijsen, Gary Tresadern
Publikováno v:
ACS Med Chem Lett
[Image: see text] Despite several years of research, only a handful of β-secretase (BACE) 1 inhibitors have entered clinical trials as potential therapeutics against Alzheimer’s disease. The intrinsic basic nature of low molecular weight, amidine-
Autor:
Carlos M. Martínez-Viturro, Colleen M. Niswender, Thomas M. Bridges, Claire Mackie, María Luz Martín-Martín, Miguel-Angel Pena, Gregor James Macdonald, Susana Conde-Ceide, Carrie K. Jones, José Manuel Bartolomé-Nebreda, Thomas Steckler, Silvia López, Han Min Tong, Hilde Lavreysen, J. Scott Daniels, Sergio A. Alonso de Diego, Jesús Alcázar, P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:429-434
As part of our efforts to identify a suitable back-up compound to our recently disclosed mGlu5 positive allosteric modulator (PAM) clinical candidate VU0490551/JNJ-46778212, this letter details the investigation and challenges of a novel series of 6,
Autor:
Carlos M. Martínez-Viturro, Colleen M. Niswender, Han Min Tong, Meredith J. Noetzel, Gregor James Macdonald, Susana Conde-Ceide, Carrie K. Jones, Claire Mackie, José Manuel Bartolomé-Nebreda, Thomas Steckler, P. Jeffrey Conn, Shaun R. Stauffer, Craig W. Lindsley, María Luz Martín-Martín, Thomas M. Bridges, J. Scott Daniels, Hilde Lavreysen, Silvia López, Sergio A. Alonso de Diego
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1310-1317
We report the discovery and SAR of two novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs). Exploration of several structural features in the western
Autor:
Gary Tresadern, Juan Antonio Vega, Andrés A. Trabanco, Encarnación Matesanz, María Lourdes Linares, José Ignacio Andrés, Claire Mackie, Gregor James Macdonald, Daniel Oehlrich, Ana Isabel de Lucas, Abdelah Ahnaou, Aránzazu García, Hilde Lavreysen, Wilhelmus Drinkenburg, José Manuel Alonso, José María Cid, Sergio A. Alonso de Diego
Publikováno v:
Journal of Medicinal Chemistry. 55:2688-2701
Advanced leads of an imidazopyridine series of positive allosteric modulators of the metabotropic glutamate 2 (mGlu2) receptor are reported. The optimization of in vitro ADMET and in vivo pharmacokinetic properties led to the identification of 27o. W
Autor:
Michiel Van Gool, Michel Surkyn, Aránzazu García-Molina, Ann Vos, Nigel Austin, Gary Tresadern, Michel Anna Jozef De Cleyn, Dieder Moechars, Carolina Martinez-Lamenca, Herman Borghys, Daniel Oehlrich, Oscar Delgado, Hana Prokopcová, Gregor James Macdonald, José Manuel Alonso, Sergio A. Alonso de Diego, Harrie J.M. Gijsen, Sven Franciscus Anna Van Brandt, Richard Alexander, Frederik J. R. Rombouts, Andrés A. Trabanco
Publikováno v:
Journal of medicinal chemistry. 58(20)
1,4-Oxazines are presented, which show good in vitro inhibition in enzymatic and cellular BACE1 assays. We describe lead optimization focused on reducing the amidine pKa while optimizing interactions in the BACE1 active site. Our strategy permitted m
Autor:
Michiel Van Gool, Francisca Delgado, Oscar Delgado, Carlos M. Martínez-Viturro, Miguel Ángel Pena, Sergio A. Alonso de Diego, Greet Vanhoof, Marta Artola, Gregor James Macdonald, José Manuel Bartolomé-Nebreda, María Luz Martín-Martín, Xavier Langlois, José Manuel Alonso, Han Min Tong, Susana Conde-Ceide, Anton Megens, Marijke Somers, Alberto Fontana
We report the continuation of a focused medicinal chemistry program aimed to further optimize a series of imidazo[1,2-a]pyrazines as a novel class of potent and selective phosphodiesterase 10A (PDE10A) inhibitors. In vitro and in vivo pharmacokinetic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::752a138a2d02674e482528380d513b5e
https://hdl.handle.net/1887/3203217
https://hdl.handle.net/1887/3203217
Autor:
M. Teresa García-López, Marta Gutiérrez-Rodríguez, Diana Frechilla, Carlos Cativiela, Rosario González-Muñiz, Edurne Cenarruzabeitia, Joaquín Del Río, Diego Casabona, M. Jesús Pérez de Vega, Rosario Herranz, Sergio A. Alonso De Diego, M. Luisa Jimeno
Publikováno v:
Digital.CSIC. Repositorio Institucional del CSIC
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A suitable solid-phase approach, based on Fmoc/tBu methodology and on the use of 2-chlorotrityl resin, allowed a rapid and efficient preparation of new GPE analogues. Most of the synthesized tripeptides displayed glutamate receptor binding affinity c
Autor:
Juan de M. Muñoz, Jesús Alcázar, Sergio-A. Alonso de Diego, Angel Díaz-Ortiz, Antonio de la Hoz
Publikováno v:
ChemInform. 43
A safe, green and functional-group-tolerant flow version of the direct amide bond formation mediated by Grignard reagents (the Bodroux reaction) is described. The procedure can be applied to a wide variety of primary and secondary amines and anilines