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

• Synthesis of pyrazole acetic acids as CRTh2 antagonists.
• Structure–activity relationships (SAR) discussed.
• Potent series of ortho-sulfonyl benzyl substituents.
• In vivo profiling of compounds 27 and 63.

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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