Search Results - "Roberts, Richard S"

Spiroindolines identify the vesicular acetylcholine transporter as a novel target for insecticide action by Sluder, Ann, Shah, Sheetal, Cassayre, Jérôme, Clover, Ralph, Maienfisch, Peter, Molleyres, Louis-Pierre, Hirst, Elizabeth A, Flemming, Anthony J, Shi, Min, Cutler, Penny, Stanger, Carole, Roberts, Richard S, Hughes, David J, Flury, Thomas, Robinson, Michael P, Hillesheim, Elke, Pitterna, Thomas, Cederbaum, Fredrik, Worthington, Paul A, Crossthwaite, Andrew J, Windass, John D, Currie, Richard A, Earley, Fergus G P

“…The efficacy of all major insecticide classes continues to be eroded by the development of resistance mediated, in part, by selection of alleles encoding…”
Get full text

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…”
Get full text

Impurity Annihilation:  Chromatography-Free Parallel Mitsunobu Reactions by Barrett, Anthony G. M, Roberts, Richard S, Schröder, Jürgen

“…Mitsunobu reaction of an alcohol ROH with a carboxylic acid, phthalimide, or N-hydroxyphthalimide (NuH) using DNAD (4) and (diphenylphosphino)polystyrene (11)…”
Get full text

2‑(Fluoromethoxy)-4′‑(S‑methanesulfonimidoyl)-1,1′-biphenyl (UCM-1306), an Orally Bioavailable Positive Allosteric Modulator of the Human Dopamine D1 Receptor for Parkinson’s Disease by García-Cárceles, Javier, Vázquez-Villa, Henar, Brea, José, Ladron de Guevara-Miranda, David, Cincilla, Giovanni, Sánchez-Martínez, Melchor, Sánchez-Merino, Anabel, Algar, Sergio, Teresa de los Frailes, María, Roberts, Richard S., Ballesteros, Juan A., Rodríguez de Fonseca, Fernando, Benhamú, Bellinda, Loza, María I., López-Rodríguez, María L.

“…Tolerance development caused by dopamine replacement with l-DOPA and therapeutic drawbacks upon activation of dopaminergic receptors with orthosteric agonists…”
Get full text

4‑Amino-7,8-dihydro-1,6-naphthyridin-5(6H)‑ones as Inhaled Phosphodiesterase Type 4 (PDE4) Inhibitors: Structural Biology and Structure–Activity Relationships by Roberts, Richard S, Sevilla, Sara, Ferrer, Manel, Taltavull, Joan, Hernández, Begoña, Segarra, Victor, Gràcia, Jordi, Lehner, Martin D, Gavaldà, Amadeu, Andrés, Miriam, Cabedo, Judit, Vilella, Dolors, Eichhorn, Peter, Calama, Elena, Carcasona, Carla, Miralpeix, Montserrat

“…Rational design of a novel template of naphthyridinones rapidly led to PDE4 inhibitors with subnanomolar enzymatic potencies. X-ray crystallography confirmed…”
Get full text

Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure–Activity Relationships by Gràcia, Jordi, Buil, Maria Antonia, Castro, Jordi, Eichhorn, Peter, Ferrer, Manel, Gavaldà, Amadeu, Hernández, Begoña, Segarra, Victor, Lehner, Martin D, Moreno, Imma, Pagès, Lluís, Roberts, Richard S, Serrat, Jordi, Sevilla, Sara, Taltavull, Joan, Andrés, Miriam, Cabedo, Judit, Vilella, Dolors, Calama, Elena, Carcasona, Carla, Miralpeix, Montserrat

“…Cyclic nucleotide cAMP is a ubiquitous secondary messenger involved in a plethora of cellular responses to biological agents involving activation of adenylyl…”
Get full text

Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists by Andrés, Miriam, Buil, Maria Antonia, Calbet, Marta, Casado, Oscar, Castro, Jordi, Eastwood, Paul R., Eichhorn, Peter, Ferrer, Manel, Forns, Pilar, Moreno, Imma, Petit, Silvia, Roberts, Richard S.

“…Pyrrolopiperidinone acetic acids (PPAs) were identified as highly potent CRTh2 receptor antagonists. In addition, many of these compounds displayed…”
Get full text

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…”
Get full text

2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists by Andrés, Miriam, Bravo, Mónica, Buil, Maria Antonia, Calbet, Marta, Castillo, Marcos, Castro, Jordi, Eichhorn, Peter, Ferrer, Manel, Lehner, Martin D., Moreno, Imma, Roberts, Richard S., Sevilla, Sara

“…In this manuscript, the synthesis and biological activity of a series of pyrazole acetic acid derivatives as CRTh2 antagonists is presented. Biological…”
Get full text

Phosphodiesterase-4 inhibitors: a review of current developments (2010 - 2012) by Gavaldà, Amadeu, Roberts, Richard S

“…At last, after many years of research, roflumilast has become the first oral phosphodiesterase-4 inhibitor to be approved by the medical agencies as an add-on…”
Get more information

Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I by Alonso, Juan Antonio, Andrés, Miriam, Bravo, Mónica, Buil, Maria Antonia, Calbet, Marta, Castro, Jordi, Eastwood, Paul R., Eichhorn, Peter, Esteve, Cristina, Gómez, Elena, González, Jacob, Mir, Marta, Petit, Silvia, Roberts, Richard S., Vidal, Bernat, Vidal, Laura, Vilaseca, Pere, Zanuy, Miriam

“…A knowledge-based design strategy led to the discovery of several new series of potent and orally bioavailable CRTh2 antagonists where a bicyclic…”
Get full text

Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists II: Lead optimization by Alonso, Juan Antonio, Andrés, Miriam, Bravo, Mónica, Calbet, Marta, Eastwood, Paul R., Eichhorn, Peter, Esteve, Cristina, Ferrer, Manel, Gómez, Elena, González, Jacob, Mir, Marta, Moreno, Imma, Petit, Silvia, Roberts, Richard S., Sevilla, Sara, Vidal, Bernat, Vidal, Laura, Vilaseca, Pere, Zanuy, Miriam

“…Extensive structure–activity relationship (SAR) and structure–kinetic relationship (SKR) studies in the bicyclic heteroaromatic series of CRTh2 antagonists led…”
Get full text

2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists by Andrés, Miriam, Bravo, Mónica, Buil, Maria Antonia, Calbet, Marta, Castro, Jordi, Domènech, Teresa, Eichhorn, Peter, Ferrer, Manel, Gómez, Elena, Lehner, Martin D., Moreno, Imma, Roberts, Richard S., Sevilla, Sara

“…High throughput screening identified the pyrazole-4-acetic acid substructure as CRTh2 receptor antagonists. Optimisation of the compounds uncovered a tight SAR…”
Get full text

ROMP-Spheres:  A Novel High-Loading Polymer Support Using Cross Metathesis between Vinyl Polystyrene and Norbornene Derivatives by Barrett, Anthony G. M, Cramp, Susan M, Roberts, Richard S

“…The preparation of a polymer-supported ruthenium alkylidene metathesis catalyst is described. This immobilized catalyst has been used to initiate a…”
Get full text

Oxazole Synthesis with Minimal Purification:  Synthesis and Application of a ROMPgel Tosmic Reagent by Barrett, Anthony G. M, Cramp, Susan M, Hennessy, Alan J, Procopiou, Panayiotis A, Roberts, Richard S

“…The synthesis of ring opening metathesis, polymer-supported Tosmic reagent 1 is described. This reagent was utilized in the conversion of aldehydes to oxazoles…”
Get full text

Horner−Emmons Synthesis with Minimal Purification Using ROMPGEL:  A Novel High-Loading Matrix for Supported Reagents by Barrett, Anthony G. M, Cramp, Susan M, Roberts, Richard S, Zecri, Frederic J

“…The synthesis and use of two novel high-loading Horner−Emmons ring-opening metathesis polymers are described. α,β-Unsaturated ethyl esters (E:Z > 99:1) and…”
Get full text

A ROMPGEL-Supported N-Hydroxysuccinimide:  A Host of Acylations with Minimal Purification by Barrett, Anthony G. M, Cramp, Susan M, Roberts, Richard S, Zecri, Frederic J

“…A novel N-hydroxysuccinimide ring-opening metathesis polymer is described as a recyclable supported acyl transfer reagent. Amides, carbamates, ureas, Weinreb…”
Get full text

ROMPGEL Scavengers:  A High-Loading Supported Anhydride for Sequestering Amines and Hydrazines by Arnauld, Thomas, Barrett, Anthony G. M, Cramp, Susan M, Roberts, Richard S, Zécri, Frederic J

“…A versatile method for sequestering excess amines and hydrazines is reported using a high-loading ROMPGEL anhydride polymer…”
Get full text

Pyrrolidine synthesis on polystyrene supports: development of a ‘one-pot’ dipolar cycloaddition strategy by Barrett, Anthony G.M, Boffey, Raymond J, Frederiksen, Mathias U, Newton, Christopher G, Roberts, Richard S

“…Preparation of substituted pyrrolidines was achieved by solid-phase synthesis via a room temperature 1,3-dipolar cycloaddition of a silver-azomethine ylide,…”
Get full text

2-(Fluoromethoxy)-4′-( S -methanesulfonimidoyl)-1,1′-biphenyl (UCM-1306), an Orally Bioavailable Positive Allosteric Modulator of the Human Dopamine D 1 Receptor for Parkinson’s Disease by García-Cárceles, Javier, Vázquez-Villa, Henar, Brea, José, Ladron de Guevara-Miranda, David, Cincilla, Giovanni, Sánchez-Martínez, Melchor, Sánchez-Merino, Anabel, Algar, Sergio, Teresa de los Frailes, María, Roberts, Richard S., Ballesteros, Juan A., Rodríguez de Fonseca, Fernando, Benhamú, Bellinda, Loza, María I., López-Rodríguez, María L.

Get full text