Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Imma Moreno"'
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:
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:
Cristina Esteve, Jacob González, Pere Vilaseca, Marta Calbet, Imma Moreno, Marta Mir, Richard S. Roberts, Silvia Petit, Elena Gómez, Mónica Bravo, Miriam Zanuy, J. A. Alonso, Manel Ferrer, Sara Sevilla, Laura Vidal, Peter Eichhorn, Miriam Andrés, Paul R. Eastwood, Bernat Vidal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:5123-5126
Extensive structure–activity relationship (SAR) and structure–kinetic relationship (SKR) studies in the bicyclic heteroaromatic series of CRTh2 antagonists led to the identification of several molecules that possessed both excellent binding and c
Autor:
Richard S. Roberts, Maria Antonia Buil, Manel Ferrer, Marcos Castillo, Miriam Andrés, Mónica Bravo, Martin D. Lehner, Jordi Castro, Sara Sevilla, Peter Eichhorn, Marta Calbet, Imma Moreno
Publikováno v:
European Journal of Medicinal Chemistry. 71:168-184
In this manuscript, the synthesis and biological activity of a series of pyrazole acetic acid derivatives as CRTh2 antagonists is presented. Biological evaluation in vitro revealed that the pyrazole core showed in several cases a different structure-
Autor:
Jordi Serrat, Jordi Gràcia, Judit Cabedo, Lluís Pagès, Dolors Vilella, Martin D. Lehner, Manel Ferrer, Montserrat Miralpeix, Peter Eichhorn, Jordi Castro, Begoña Hernández, Maria Antonia Buil, Victor Segarra, Elena Calama, Sara Sevilla, Carla Carcasona, Miriam Andrés, Joan Taltavull, Imma Moreno, Richard S. Roberts, Amadeu Gavaldà
Publikováno v:
Journal of medicinal chemistry. 59(23)
Cyclic nucleotide cAMP is a ubiquitous secondary messenger involved in a plethora of cellular responses to biological agents involving activation of adenylyl cyclase. Its intracellular levels are tightly controlled by a family of cyclic nucleotide de
Discovery of a novel class of zwitterionic, potent, selective and orally active S1P1 direct agonists
Autor:
Gema Tarrasón, Nuria Godessart, Marta Mir, Clara Armengol, Mònica Córdoba, Dolors Vilella, Daniel Casals, Manel López, Victor Segarra, Teresa Doménech, Imma Moreno, M Sabate, Nuria Aguilar, Pedro M. Grima, María Domínguez, Laia Esteban
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7672-7676
Amido-1,3,4-thiadiazoles have been identified as a novel structural class of potent and selective sphingosine-1-phosphate receptor subtype 1 agonists. Starting from a micromolar HTS hit with the help of an in-house homology model, robust structural
Autor:
Jordi Sanahuja, Montse Erra, Nuria Godessart, Raquel F. Reinoso, Estrella Lozoya, Imma Moreno, Pilar Pizcueta, Julio C. Castro-Palomino, Miriam Andrés
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:7268-7272
The structure–activity relationships of a novel series of biaryl dihydroorotate dehydrogenase (DHODH) inhibitors related to teriflunomide are disclosed. These biaryl derivatives were the result of structure-based design and proved to be potent DHOD
Autor:
Angel F. Remacha, M. Arilla, Imma Moreno, Neus Boto, Adelaida Ramos, Jorge Sierra, Rodrigo Martino, Concepción Pastoret, P Madoz, Clara Martínez, E Muniz-Diaz, C. Canals
Publikováno v:
Transfusion. 44:1603-1611
BACKGROUND: Most studies indicate that ABO incompatibility has no effect on the clinical outcome after allogeneic peripheral blood progenitor cell (PBPC) transplantation (allo-PBPCT). However, it carries additional risks of hemolytic reactions, delay
Autor:
Martin D. Lehner, Teresa Doménech, Imma Moreno, Elena Gómez, Jordi Castro, Maria Antonia Buil, Manel Ferrer, Miriam Andrés, Sara Sevilla, Marta Calbet, Mónica Bravo, Peter Eichhorn, Richard S. Roberts
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(11)
High throughput screening identified the pyrazole-4-acetic acid substructure as CRTh2 receptor antagonists. Optimisation of the compounds uncovered a tight SAR but also identified some low nanomolar inhibitors.
Discovery of a novel class of zwitterionic, potent, selective and orally active S1P₁ direct agonists
Autor:
Nuria, Aguilar, Marta, Mir, Pedro M, Grima, Manel, López, Victor, Segarra, Laia, Esteban, Imma, Moreno, Nuria, Godessart, Gema, Tarrasón, Teresa, Domenech, Dolors, Vilella, Clara, Armengol, Mònica, Córdoba, Mar, Sabaté, Daniel, Casals, Maria, Domínguez
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(24)
Amido-1,3,4-thiadiazoles have been identified as a novel structural class of potent and selective sphingosine-1-phosphate receptor subtype 1 agonists. Starting from a micromolar HTS hit with the help of an in-house homology model, robust structural-a