title: 2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists.
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.
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Miriam
authors.initials: M
authors.lastname: Andrés
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Mónica
authors.initials: M
authors.lastname: Bravo
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Maria Antonia
authors.initials: MA
authors.lastname: Buil
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Marta
authors.initials: M
authors.lastname: Calbet
authors.affiliation: Almirall-Barcelona Science Park Unit, Barcelona Science Park, Baldiri Reixac 10, 08028 Barcelona, Spain.
authors.forename: Marcos
authors.initials: M
authors.lastname: Castillo
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Jordi
authors.initials: J
authors.lastname: Castro
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Peter
authors.initials: P
authors.lastname: Eichhorn
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Manel
authors.initials: M
authors.lastname: Ferrer
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Martin D
authors.initials: MD
authors.lastname: Lehner
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Imma
authors.initials: I
authors.lastname: Moreno
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain. Electronic address: rick.roberts@almirall.com.
authors.forename: Richard S
authors.initials: RS
authors.lastname: Roberts
authors.affiliation: Almirall R&D Centre, Laureano Miró 408-410, 08980 Sant Feliu de Llobregat, Barcelona, Spain.
authors.forename: Sara
authors.initials: S
authors.lastname: Sevilla
mesh_terms: D000085:Acetates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000085:Acetates; D011720:Pyrazoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C031280:pyrazole; C036293:prostaglandin D2 receptor
keywords: CRTh2 antagonists; Pyrazole; Structure–activity relationship (SAR)