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ID: ALA3098073

Journal: Eur J Med Chem

Title: 2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists.

Authors: Andrés M, Bravo M, Buil MA, Calbet M, Castillo M, Castro J, Eichhorn P, Ferrer M, Lehner MD, Moreno I, Roberts RS, Sevilla S.

Abstract: 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 showed in several cases a different structure-activity relationship (SAR) to that of related indole acetic acid. A potent series of ortho-sulfonyl benzyl substituents was found, from which compounds 27 and 63 were advanced to in vivo profiling.

CiteXplore: 24292338

DOI: 10.1016/j.ejmech.2013.10.072