2-(1H-Pyrazol-1-yl) acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists
…, M Calbet, M Castillo, J Castro, P Eichhorn…
Index: Andres, Miriam; Bravo, Monica; Buil, Maria Antonia; Calbet, Marta; Castillo, Marcos; Castro, Jordi; Eichhorn, Peter; Ferrer, Manel; Lehner, Martin D.; Moreno, Imma; Roberts, Richard S.; Sevilla, Sara European Journal of Medicinal Chemistry, 2014 , vol. 71, p. 168 - 184
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Citation Number: 6
Abstract
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 ...
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