2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists

Miriam Andrés; Mónica Bravo; Maria Antonia Buil; Marta Calbet; Jordi Castro; Teresa Domènech; Peter Eichhorn; Manel Ferrer; Elena Gómez; Martin D Lehner; Imma Moreno; Richard S Roberts; Sara Sevilla

doi:10.1016/j.bmcl.2013.03.093

2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3349-53. doi: 10.1016/j.bmcl.2013.03.093. Epub 2013 Apr 2.

Authors

Miriam Andrés¹, Mónica Bravo, Maria Antonia Buil, Marta Calbet, Jordi Castro, Teresa Domènech, Peter Eichhorn, Manel Ferrer, Elena Gómez, Martin D Lehner, Imma Moreno, Richard S Roberts, Sara Sevilla

Affiliation

¹ Almirall R&D Centre, Laureano Miró, 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.

PMID: 23601708
DOI: 10.1016/j.bmcl.2013.03.093

Abstract

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.

MeSH terms

Acetates / chemical synthesis
Acetates / chemistry*
Acetates / pharmacokinetics
Animals
Half-Life
High-Throughput Screening Assays
Protein Binding
Pyrazoles / chemistry*
Rats
Receptors, Immunologic / antagonists & inhibitors*
Receptors, Immunologic / metabolism
Receptors, Prostaglandin / antagonists & inhibitors*
Receptors, Prostaglandin / metabolism
Structure-Activity Relationship

Substances

Acetates
Pyrazoles
Receptors, Immunologic
Receptors, Prostaglandin
pyrazole
prostaglandin D2 receptor