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.
Miriam Andrés  1 ,  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
Affiliations
  • 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.

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