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2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2)
Miriam Andrés1, Mónica Bravo1, Maria Antonia Buil1
1Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
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.
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