Zobrazeno 1 - 10
of 45
pro vyhledávání: '"A. Pilar Forns"'
Autor:
Laura Vidal, Miriam Andrés, Marta Mir, Pilar Forns, Sara Sevilla, Bernat Vidal, Estrella Lozoya, Cristina Esteve, Mónica Bravo, Manel Ferrer, Paul R. Eastwood, Richard S. Roberts, Jordi Castro, Elena Gómez, Marta Calbet, Pere Vilaseca, Jacob González, Imma Moreno, Silvia Petit, J. A. Alonso, Maria Antonia Buil
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:5127-5133
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 long receptor residence time. The HBA in combination with a small steric substituent in the
Autor:
Richard S. Roberts, Maria Antonia Buil, Peter Eichhorn, Paul R. Eastwood, Imma Moreno, Silvia Petit, Pilar Forns, Jordi Castro, Oscar Casado, Manel Ferrer, Miriam Andrés, Marta Calbet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:5111-5117
Pyrrolopiperidinone acetic acids (PPAs) were identified as highly potent CRTh2 receptor antagonists. In addition, many of these compounds displayed slow-dissociation kinetics from the receptor. Structure–kinetic relationship (SKR) studies allowed o
Autor:
Montserrat Miralpeix, Manel López, Marcos Castillo, Montse Erra, Adelina Orellana, Bernat Vidal, Marta Mir, Pilar Forns, Isabel Ramis, M. I. Maldonado, Cristina Carreño
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5419-5423
A novel class of potent Syk inhibitors has been developed from rational design. Highly potent aminopyridine derivatives bearing a 4-trifluoromethyl-2-pyridyl motif and represented by compound 13b IC50: 0.6 nM were identified. Substitution by a 2-pyra
Autor:
Bernat Vidal, Lorena Taboada, MA López, Cristina Esteve, Pilar Forns, Montserrat Miralpeix, J. A. Alonso, Isabel Ramis, Adelina Orellana, Cristina Carreño, M. I. Maldonado
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2784-2788
A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular a
Autor:
Pere Vilaseca, Marcos Castillo, Bernat Vidal, Cristina Esteve, Richard S. Roberts, Sara Sevilla, Manel Ferrer, Maria Antonia Buil, Jordi Castro, Sara López, Marta Calbet, Laura Vidal, Pilar Forns, Jacob González
Publikováno v:
European journal of medicinal chemistry. 113
Monocyclic and bicyclic ring systems were investigated as the "core" section of a series of diphenylsulphone-containing acetic acid CRTh2 receptor antagonists. A range of potencies were observed and single-digit nanomolar potencies were obtained in b
Autor:
Joan-Carles Fernàndez, Natalia de la Figuera, Paul R. Eastwood, Sandra Fiol, Fernando Albericio, Pilar Forns
Publikováno v:
QSAR & Combinatorial Science. 27:1267-1273
The immobilization and reactions of indazol-3-carboxylic acid on the solid phase is described. These reactions are of importance since many biologically active compounds contain an indazole core. Here, indazole 3-carboxylic acid was efficiently ancho
Autor:
Pilar Forns, Dolors Fernández-Forner, Natalia de la Figuera, Fernando Albericio, Joan C. Fernandez, Sandra Fiol
Publikováno v:
Letters in Organic Chemistry. 5:374-378
Autor:
Fernando Albericio, Joan-Carles Fernàndez, Aina Colombo, Natalia de la Figuera, Pilar Forns, Dolors Fernández-Forner
Publikováno v:
Tetrahedron Letters. 49:1569-1572
Diastereoselectivity in the oxidation of different 4-thiazolidinones was discussed. Alkylation of these compounds with benzyl bromide was also studied. The stereoselectivity obtained was interpreted by the presence of the sulfoxide.
Autor:
Fernando Albericio, Joan-Carles Fernàndez, Natalia de la Figuera, Pilar Forns, Dolors Fernández-Forner, Aina Colombo
Publikováno v:
Organic Letters. 9:4319-4322
Synthesis and applications of two new nonacid degradable linkers as an alternative to the Wang linker for solid-phase synthesis are described. Resin from linker 2 looks superior to linker 1 in terms of yields for both anchoring of the first building
Publikováno v:
Tetrahedron: Asymmetry. 17:3327-3331
The asymmetric oxidation of a sulfide in the solid phase using two distinct scaffolds as models is described.