Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Carlos M. Martínez-Viturro"'
Autor:
Francisca Delgado, Jordi Royes, Alcira del Cerro, Fulgencio Tovar, Juan Antonio Vega, Paul Shaffer, Andrés A. Trabanco, Elena Fernández, Alexis Bretteville, Gary Tresadern, Andreas Ebneth, José Manuel Bartolomé-Nebreda, Carlos M Martínez-Viturro, Liesbeth Mertens, Marijke Somers, Aránzazu García Molina, José Manuel Alonso
Publikováno v:
Journal of Medicinal Chemistry. 63:14017-14044
O-GlcNAcylation is a post-translational modification of tau understood to lower the speed and yield of its aggregation, a pathological hallmark of Alzheimer's disease (AD). O-GlcNAcase (OGA) is the only enzyme that removes O-linked N-acetyl-d-glucosa
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:
José Manuel Bartolomé-Nebreda, Thomas Steckler, Susana Conde-Ceide, Colleen M. Niswender, Chrysa Malosh, María Piedrafita, Meredith J. Noetzel, Claire Mackie, Paige N. Vinson, Jerri M. Rook, Gregor James Macdonald, M. Rosa Sánchez-Casado, P. Jeffrey Conn, Shaun R. Stauffer, Carlos M. Martínez-Viturro, Hilde Lavreysen, J. Scott Daniels, Carrie K. Jones, Mark Turlington, Thomas M. Bridges, Craig W. Lindsley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5115-5120
We report the optimization of a series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) from an acyl dihydropyrazolo[1,5-a]pyrimidinone class. Investigation of exocyclic amide transpositions with this unique 5,6-bicy
Autor:
Susana Conde-Ceide, Craig W. Lindsley, P. Jeffrey Conn, Gregor James Macdonald, Colleen M. Niswender, J. Scott Daniels, Claire Mackie, Ya Zhou, José Manuel Bartolomé-Nebreda, Thomas Steckler, Chrysa Malosh, Carlos M. Martínez-Viturro, Jesús Alcázar, Thomas M. Bridges, Hilde Lavreysen, Shaun R. Stauffer, Carrie K. Jones
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3515-3519
This Letter describes the progress and challenges in the continued optimization of the mGlu5 positive allosteric modulator (PAM) clinical candidate VU0490551/JNJ-46778212. While many analogs addressed key areas for improvement, no one compound posses
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:
José Manuel Bartolomé-Nebreda, Marijke Somers, Laura Iturrino, Greet Vanhoof, Joaquín Pastor, Susana Conde-Ceide, María Luz Martín-Martín, Xavier Langlois, Gregor James Macdonald, Anton Megens, Francisca Delgado, Wendy Sanderson, Carlos M. Martínez-Viturro, Han Min Tong
Publikováno v:
Journal of Medicinal Chemistry. 57:4196-4212
We report the discovery of a series of imidazo[1,2-a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10A (PDE10A). In a high-throughput screening campaign we identified the imidazopyrazine derivative 1, a PDE10A inhibitor with limited s
Autor:
Hilde Lavreysen, P. Jeffrey Conn, Xavier Langlois, José Manuel Bartolomé-Nebreda, Thomas Steckler, Jerri M. Rook, Paige N. Vinson, Gregor James Macdonald, Craig W. Lindsley, Anton Megens, Jesús Alcázar, J. Scott Daniels, Carrie K. Jones, Colleen M. Niswender, Pedro M. Garcia-Barrantes, Thomas M. Bridges, Wilhelmus Drinkenburg, A. Ahnaou, Shaun R. Stauffer, Carlos M. Martínez-Viturro, Susana Conde-Ceide, Claire Mackie
Publikováno v:
ACS medicinal chemistry letters. 6(6)
Herein, we report the structure–activity relationship of a novel series of (2(phenoxymethyl)-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-yl(aryl)methanones as potent, selective, and orally bioavailable metabotropic glutamate receptor subtype 5 (mGlu5)
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