Search Results - "Vidal, Bernat"

Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists III: The role of a hydrogen-bond acceptor in long receptor residence times by Alonso, Juan Antonio, Andrés, Miriam, Bravo, Mónica, Buil, Maria Antonia, Calbet, Marta, Castro, Jordi, Eastwood, Paul R., Esteve, Cristina, Ferrer, Manel, Forns, Pilar, Gómez, Elena, González, Jacob, Lozoya, Estrella, Mir, Marta, Moreno, Imma, Petit, Silvia, Roberts, Richard S., Sevilla, Sara, Vidal, Bernat, Vidal, Laura, Vilaseca, Pere

“…The correct positioning and orientation of an hydrogen bond acceptor (HBA) in the tail portion of the biaryl series of CRTh2 antagonists is a requirement for…”
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Reelin delays amyloid-beta fibril formation and rescues cognitive deficits in a model of Alzheimer’s disease by Pujadas, Lluís, Rossi, Daniela, Andrés, Rosa, Teixeira, Cátia M., Serra-Vidal, Bernat, Parcerisas, Antoni, Maldonado, Rafael, Giralt, Ernest, Carulla, Natàlia, Soriano, Eduardo

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Design, Synthesis, and Structure−Activity Relationships of 1-,3-,8-, and 9-Substituted-9-deazaxanthines at the Human A2B Adenosine Receptor by Carotti, Angelo, Cadavid, Maria Isabel, Centeno, Nuria B, Esteve, Cristina, Loza, Maria Isabel, Martinez, Ana, Nieto, Rosa, Raviña, Enrique, Sanz, Ferran, Segarra, Victor, Sotelo, Eddy, Stefanachi, Angela, Vidal, Bernat

“…Over two hundred 1-, 3-, 8-, and 9-substituted-9-deazaxanthines were prepared and evaluated for their binding affinity at the recombinant human adenosine…”
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A new chemical tool (C0036E08) supports the role of adenosine A2B receptors in mediating human mast cell activation by BUCETA, Montserrat, DOMINGUEZ, Eduardo, DIAZ, Jose Luis, MIRALPEIX, Montse, BELETA, Jorge, CADAID, Maria Isabel, LOZA, Maria Isabel, CASTRO, Marian, BREA, José, ALVAREZ, David, BARCALA, Javier, VALDES, Luis, ALVAREZ-CALDERON, Pedro, DOMINGUEZ, Femando, VIDAL, Bernat

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Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist by Eastwood, Paul, Esteve, Cristina, González, Jacob, Fonquerna, Silvia, Aiguadé, Josep, Carranco, Inés, Doménech, Teresa, Aparici, Mònica, Miralpeix, Montserrat, Albertí, Joan, Córdoba, Mónica, Fernández, Raquel, Pont, Mercè, Godessart, Núria, Prats, Neus, Loza, María Isabel, Cadavid, María Isabel, Nueda, Arsenio, Vidal, Bernat

“…The structure−activity relationships for a series of pyrazine-based A2B adenosine receptor antagonists are described. From this work, LAS101057 (17), a potent,…”
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Nucleophilic Addition of 1-Acetylindole Enolates to Pyridinium Salts. Stereoselective Formal Synthesis of (±)-Geissoschizine and (±)-Akagerine via 1,4-Dihydropyridines by Bennasar, M.-Lluïsa, Jiménez, Juan-Miguel, Vidal, Bernat, Sufi, Bilal A, Bosch, Joan

“…Addition of the enolate derived from 1-acetylindole (3) to pyridinium salt 4b followed by acid-induced cyclization of the resulting 1,4-dihydropyridine 5b in…”
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Reelin delays amyloid-beta fibril formation and rescues cognitive deficits in a model of Alzheimer’s disease by Pujadas, Lluís, Rossi, Daniela, Andrés, Rosa, Teixeira, Cátia M., Serra-Vidal, Bernat, Parcerisas, Antoni, Maldonado, Rafael, Giralt, Ernest, Carulla, Natàlia, Soriano, Eduardo

“…Reelin is an extracellular matrix protein that is crucial for neural development and adult brain plasticity. While the Reelin signalling cascade has been…”
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Prediction of the skin permeability of topical drugs using in silico and in vitro models by Alonso, Cristina, Carrer, Víctor, Espinosa, Sonia, Zanuy, Miriam, Córdoba, Mònica, Vidal, Bernat, Domínguez, María, Godessart, Núria, Coderch, Luisa, Pont, Mercè

“…The main challenge of topically applied drugs is to overcome the skin barrier to reach the site of action at the concentration needed for efficacy. In the…”
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Addition of chiral enolates to N-alkyl-3-acylpyridinium salts. Total synthesis of (+)-16-epivinoxine and (−)-vinoxine by Bennasar, M.-Lluı̈sa, Zulaica, Ester, Alonso, Yolanda, Vidal, Bernat, Vázquez, Jesús T., Bosch, Joan

“…Chiral enolates of indolylacetyl derivatives 6a– f undergo addition to pyridinium salt 7 with complete trans-selectivity and varied diastereofacial…”
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Nucleophilic Addition of 2-Acetylindole Enolates to Pyridinium Salts. Acylation of the Intermediate Dihydropyridines by Bennasar, M.-Lluiesa, Vidal, Bernat, Bosch, Joan

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A novel inhaled Syk inhibitor blocks mast cell degranulation and early asthmatic response by Ramis, Isabel, Otal, Raquel, Carreño, Cristina, Domènech, Anna, Eichhorn, Peter, Orellana, Adelina, Maldonado, Mónica, De Alba, Jorge, Prats, Neus, Fernández, Joan-Carles, Vidal, Bernat, Miralpeix, Montserrat

“…Spleen tyrosine kinase (Syk) is essential for signal transduction of immunoreceptors. Inhibition of Syk abrogates mast cell degranulation and B cell responses…”
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Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma by Esteve, Cristina, González, Jacob, Gual, Sílvia, Vidal, Laura, Alzina, Soledad, Sentellas, Sonia, Jover, Irene, Horrillo, Raquel, De Alba, Jorge, Miralpeix, Montserrat, Tarrasón, Gema, Vidal, Bernat

“…[Display omitted] Synthesis and SAR of a series of 7-azaindoles as Orai channel inhibitors showing good potency inhibiting IL-2 production in Jurkat cells is…”
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Hydrogen/Deuterium Exchange-Protected Oligomers Populated during Aβ Fibril Formation Correlate with Neuronal Cell Death by Serra-Vidal, Bernat, Pujadas, Lluís, Rossi, Daniela, Soriano, Eduardo, Madurga, Sergio, Carulla, Natàlia

“…The aggregation of the amyloid-β peptide (Aβ) to form fibrils and plaques is strongly associated with Alzheimer’s disease (AD). Although it is well established…”
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Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists by Buil, Maria Antonia, Calbet, Marta, Castillo, Marcos, Castro, Jordi, Esteve, Cristina, Ferrer, Manel, Forns, Pilar, González, Jacob, López, Sara, Roberts, Richard S., Sevilla, Sara, Vidal, Bernat, Vidal, Laura, Vilaseca, Pere

“…Monocyclic and bicyclic ring systems were investigated as the “core” section of a series of diphenylsulphone-containing acetic acid CRTh2 receptor antagonists…”
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First synthesis of pyrrolothiadiazinones. An alternative core ring for xanthine based structures by Esteve, Cristina, Vidal, Bernat

“…A straightforward synthesis of novel condensed pyrrolothiadiazines is described. The first synthesis of pyrrolothiadiazine core ring bearing substituents at…”
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Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A2B adenosine receptor antagonists by EASTWOOD, Paul, GONZALEZ, Jacob, PAREDES, Sergio, NUEDA, Arsenio, DOMENECH, Teresa, ALBERTI, Joan, VIDAL, Bernat

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Indolin-2-one p38α inhibitors I: Design, profiling and crystallographic binding mode by Eastwood, Paul, González, Jacob, Gómez, Elena, Vidal, Bernat, Caturla, Francisco, Roca, Ramón, Balagué, Cristina, Orellana, Adelina, Domínguez, María

“…The use of structure-based design and molecular modeling led to the discovery of indolin-2-one derivatives as potent and selective p38α inhibitors. The use of…”
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Highly potent aminopyridines as Syk kinase inhibitors by Castillo, Marcos, Forns, Pilar, Erra, Montse, Mir, Marta, López, Manel, Maldonado, Mónica, Orellana, Adelina, Carreño, Cristina, Ramis, Isabel, Miralpeix, Montserrat, Vidal, Bernat

“…A novel class of potent Syk inhibitors has been developed from rational design. Highly potent aminopyridine derivatives bearing a 4-trifluoromethyl-2-pyridyl…”
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1,7-Naphthyridine 1-Oxides as Novel Potent and Selective Inhibitors of p38 Mitogen Activated Protein Kinase by Lumeras, Wenceslao, Vidal, Laura, Vidal, Bernat, Balagué, Cristina, Orellana, Adelina, Maldonado, Mónica, Domínguez, María, Segarra, Víctor, Caturla, Francisco

“…The design, synthesis, and ability to inhibit p38α MAP kinase by a novel series of naphthyridine N-oxides will be described. Some of these compounds showed a…”
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Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists by Eastwood, Paul, Gonzalez, Jacob, Paredes, Sergio, Nueda, Arsenio, Domenech, Teresa, Alberti, Joan, Vidal, Bernat

“…The synthesis and SAR of a series of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent A(2B) adenosine receptor antagonists is described. Several compounds…”
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