Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Susana Conde Ceide"'
Autor:
Hilde Lavreysen, Ivan R. Torrecillas, Susana Conde-Ceide, Ana Isabel de Lucas, Andrés A. Trabanco, Gary Tresadern, Leonardo Pardo, Aránzazu García Molina
Publikováno v:
ACS chemical neuroscience. 10(5)
Experiment and modeling were combined to understand inhibition of the alanine-serine-cysteine-1 (asc1) transporter. The structure-activity relationship (SAR) was explored with synthesis of analogues of BMS-466442. Direct target interaction and bindin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::39d6b8f3618e49e184c1179a2bcdb705
https://pubmed.ncbi.nlm.nih.gov/30821959
https://pubmed.ncbi.nlm.nih.gov/30821959
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,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c3b86aa42123689c0f8547589986f3f
https://doi.org/10.1016/j.bmcl.2015.11.098
https://doi.org/10.1016/j.bmcl.2015.11.098
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b8088322559a22014da4ba8a0d907b9
https://doi.org/10.1016/j.bmcl.2015.10.009
https://doi.org/10.1016/j.bmcl.2015.10.009
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7441129eb76aa61e9831657c5e991b6
https://doi.org/10.1016/j.bmcl.2015.06.096
https://doi.org/10.1016/j.bmcl.2015.06.096
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4a364a4c4741589a3db21524a2a658a
https://doi.org/10.1016/j.bmcl.2015.01.038
https://doi.org/10.1016/j.bmcl.2015.01.038
Autor:
Shaun R. Stauffer, Thomas M. Bridges, J. Scott Daniels, Meredith J. Noetzel, Hilde Lavreysen, Colleen M. Niswender, Craig W. Lindsley, P. Jeffrey Conn, Han Min Tong, Susana Conde-Ceide, José Manuel Bartolomé-Nebreda, Thomas Steckler, Carrie K. Jones, Paige N. Vinson, Gregor James Macdonald, Claire Mackie, Mark Turlington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3641-3646
We report the optimization of a series of novel metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) from a 5,6-bicyclic class of dihydropyrazolo[1,5-a]pyridin-4(5H)-ones containing a phenoxymethyl linker. Studies focused o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::570caf0830a9486752156fe572e3bde1
https://doi.org/10.1016/j.bmcl.2014.04.087
https://doi.org/10.1016/j.bmcl.2014.04.087
Autor:
Jason Manka, Hilde Lavreysen, Colleen M. Niswender, Jon Jacobs, M. Luz Martín-Martín, P. Jeffrey Conn, Meredith J. Noetzel, Han Min Tong, Elizabeth J. Herman, C. David Weaver, Chrysa Malosh, J. Scott Daniels, Susana Conde-Ceide, Paige N. Vinson, Shaun R. Stauffer, Gregor James Macdonald, Claire Mackie, José Manuel Bartolomé-Nebreda, Thomas Steckler, Silvia López, Craig W. Lindsley, Carrie K. Jones, Satyawan Jadhav, Mark Turlington
Publikováno v:
Journal of Medicinal Chemistry. 57:5620-5637
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGlu5) represent a promising therapeutic strategy for the treatment of schizophrenia. Starting from an acetylene-based lead from high throughput screening, an evolved bicycli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ec9e09891e97fb3e6b29c5a56f045fdf
https://doi.org/10.1021/jm500259z
https://doi.org/10.1021/jm500259z
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12ac9ae359ff0523ce350342854294aa
https://doi.org/10.1021/jm500073h
https://doi.org/10.1021/jm500073h
Autor:
Zhijun Wang, Erik Boman, Jan Urban, Jeff Kucharski, Hiroshi Nakanishi, Jan Lundström, Nancy G. J. Delaet, Justin T. Ernst, Eddine Saiah, Christopher Lum, Eric Erb, Antonio Garrido Montalban, Susana Conde Ceide, Russell Dahl, Linda Kessler, Stephen E. Miller, Christopher J. Larson, Chau-Dung Chang, Edward Roberts, Jeffrey Kahl, Robert K. P. Sullivan, Andrew Gibbs, David Dalesandro
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4819-4824
We have optimized a novel series of potent p38 MAP kinase inhibitors based on an alpha-ketoamide scaffold through structure based design that due to their extended molecular architecture bind, in addition to the ATP site, to an allosteric pocket. In
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::646db32d2692e24d80d296daacfeccd7
https://doi.org/10.1016/j.bmcl.2010.06.102
https://doi.org/10.1016/j.bmcl.2010.06.102
Autor:
Jan Lundström, Eric Erb, Susana Conde Ceide, Eddine Saiah, Jeff Kahl, Stephen E. Miller, Andrew Gibbs, Edward Roberts, Nancy G. J. Delaet, Antonio Garrido Montalban, Robert K. P. Sullivan, Erik Boman, Zhijun Wang, Christopher J. Larson, David Dalesandro, Russell Dahl, Chau-Dung Chang, Hiroshi Nakanishi, Linda Kessler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5456-5459
We have identified a second series of potent p38 inhibitors. As with our first generation series, these compounds are based on an alpha-ketoamide scaffold. The reversal of the ketoamide order, however, introduces more chemical flexibility and in addi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df8879f4a8eb58917957fc3b2d5d8d5e
https://doi.org/10.1016/j.bmcl.2008.09.028
https://doi.org/10.1016/j.bmcl.2008.09.028