Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists
Maria Antonia Buil
1
,
Marta Calbet
1
,
Marcos Castillo
2
,
Jordi Castro
1
,
Cristina Esteve
1
,
Manel Ferrer
1
,
Pilar Forns
2
,
Jacob González
1
,
Sara Lopez
1
,
Richard S. Roberts
1
,
Sara Sevilla
1
,
Bernat Vidal
1
,
Laura Vidal
1
,
Pere Vilaseca
1
1
Almirall R&D Centre, Laureano Miró, 408-410, 08980, Sant Feliu de Llobregat, Barcelona, Spain.
|
2
Almirall-Barcelona Science Park Unit, Barcelona Science Park, Josep Samitier 1-5, 08028 Barcelona, Spain.
|
Publication type: Journal Article
Publication date: 2016-05-01
scimago Q1
wos Q1
SJR: 1.142
CiteScore: 11.3
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
26922232
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Abstract
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 both the monocyclic and bicyclic cores. Residence times for the monocyclic compounds were very short. Some of the bicyclic cores displayed better residence times. A methyl group in the northern part of the core, between the head and tail was a necessary requirement for the beginnings of long residence times. Variations of the tail substitution maximised potencies and residence times.
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Total citations:
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Citations from 2024:
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(17.64%)
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Buil M. A. et al. Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists // European Journal of Medicinal Chemistry. 2016. Vol. 113. pp. 102-133.
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Buil M. A., Calbet M., Castillo M., Castro J., Esteve C., Ferrer M., Forns P., González J., Lopez S., Roberts R. S., Sevilla S., Vidal B., Vidal L., Vilaseca P. Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists // European Journal of Medicinal Chemistry. 2016. Vol. 113. pp. 102-133.
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TY - JOUR
DO - 10.1016/j.ejmech.2016.02.023
UR - https://doi.org/10.1016/j.ejmech.2016.02.023
TI - Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists
T2 - European Journal of Medicinal Chemistry
AU - Buil, Maria Antonia
AU - Calbet, Marta
AU - Castillo, Marcos
AU - Castro, Jordi
AU - Esteve, Cristina
AU - Ferrer, Manel
AU - Forns, Pilar
AU - González, Jacob
AU - Lopez, Sara
AU - Roberts, Richard S.
AU - Sevilla, Sara
AU - Vidal, Bernat
AU - Vidal, Laura
AU - Vilaseca, Pere
PY - 2016
DA - 2016/05/01
PB - Elsevier
SP - 102-133
VL - 113
PMID - 26922232
SN - 0223-5234
SN - 1768-3254
ER -
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BibTex (up to 50 authors)
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@article{2016_Buil,
author = {Maria Antonia Buil and Marta Calbet and Marcos Castillo and Jordi Castro and Cristina Esteve and Manel Ferrer and Pilar Forns and Jacob González and Sara Lopez and Richard S. Roberts and Sara Sevilla and Bernat Vidal and Laura Vidal and Pere Vilaseca},
title = {Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists},
journal = {European Journal of Medicinal Chemistry},
year = {2016},
volume = {113},
publisher = {Elsevier},
month = {may},
url = {https://doi.org/10.1016/j.ejmech.2016.02.023},
pages = {102--133},
doi = {10.1016/j.ejmech.2016.02.023}
}