Richard S Roberts
Overview
Explore the profile of Richard S Roberts including associated specialties, affiliations and a list of published articles.
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13
Citations
50
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Recent Articles
1.
Garcia-Carceles J, Vazquez-Villa H, Brea J, de Guevara-Miranda D, Cincilla G, Sanchez-Martinez M, et al.
J Med Chem
. 2022 Aug;
65(18):12256-12272.
PMID: 36044544
Tolerance development caused by dopamine replacement with l-DOPA and therapeutic drawbacks upon activation of dopaminergic receptors with orthosteric agonists reveal a significant unmet need for safe and effective treatment of...
2.
Roberts R, Sevilla S, Ferrer M, Taltavull J, Hernandez B, Segarra V, et al.
J Med Chem
. 2018 Mar;
61(6):2472-2489.
PMID: 29502405
Rational design of a novel template of naphthyridinones rapidly led to PDE4 inhibitors with subnanomolar enzymatic potencies. X-ray crystallography confirmed the binding mode of this novel template. We achieved compounds...
3.
Gracia J, Buil M, Castro J, Eichhorn P, Ferrer M, Gavalda A, et al.
J Med Chem
. 2016 Dec;
59(23):10479-10497.
PMID: 27933955
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...
4.
Buil M, Calbet M, Castillo M, Castro J, Esteve C, Ferrer M, et al.
Eur J Med Chem
. 2016 Feb;
113:102-33.
PMID: 26922232
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...
5.
Alonso J, Andres M, Bravo M, Buil M, Calbet M, Castro J, et al.
Bioorg Med Chem Lett
. 2014 Dec;
24(21):5127-33.
PMID: 25437506
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....
6.
Alonso J, Andres M, Bravo M, Calbet M, Eastwood P, Eichhorn P, et al.
Bioorg Med Chem Lett
. 2014 Dec;
24(21):5123-6.
PMID: 25437505
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...
7.
Alonso J, Andres M, Bravo M, Buil M, Calbet M, Castro J, et al.
Bioorg Med Chem Lett
. 2014 Dec;
24(21):5118-22.
PMID: 25437504
A knowledge-based design strategy led to the discovery of several new series of potent and orally bioavailable CRTh2 antagonists where a bicyclic heteroaromatic ring serves as the central core. Structure-kinetic...
8.
Andres M, Buil M, Calbet M, Casado O, Castro J, Eastwood P, et al.
Bioorg Med Chem Lett
. 2014 Dec;
24(21):5111-7.
PMID: 25437503
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 optimisation...
9.
Andres M, Bravo M, Buil M, Calbet M, Castillo M, Castro J, et al.
Eur J Med Chem
. 2013 Dec;
71:168-84.
PMID: 24292338
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...
10.
Gavalda A, Roberts R
Expert Opin Ther Pat
. 2013 May;
23(8):997-1016.
PMID: 23642007
Introduction: 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 therapy for chronic obstructive...