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Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists. 2016
Maria Antonia Buil, and
Marta Calbet, and
Marcos Castillo, and
Jordi Castro, and
Cristina Esteve, and
Manel Ferrer, and
Pilar Forns, and
Jacob González, and
Sara López, and
Richard S Roberts, and
Sara Sevilla, and
Bernat Vidal, and
Laura Vidal, and
Pere Vilaseca
Almirall R&D Centre, Laureano Miró, 408-410, 08980, Sant Feliu de Llobregat, Barcelona, Spain.
Monocyclic and bicyclic ring systems were investigated as the "core" section of a series of diphenylsulphone-containing acetic acid CRTh2 receptor antagonists. A range of potencies were observed and single-digit nanomolar potencies were obtained in both the monocyclic and bicyclic cores. Residence times for the monocyclic compounds were very short. Some of the bicyclic cores displayed better residence times. A methyl group in the northern part of the core, between the head and tail was a necessary requirement for the beginnings of long residence times. Variations of the tail substitution maximised potencies and residence times.
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