2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists

High throughput screening identified a phenoxyacetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a compound with functional potency for inhibition of human eosinophil shape change and oral bioavailability in the rat.

High throughput screening identified a phenoxyacetic acid scaffold 3 as a novel CRTh2 receptor antagonist chemotype. Optimisation furnished compound 6b, which showed functional potency for inhibition of human eosinophil shape change and oral bioavailability in the rat.Figure optionsDownload as PowerPoint slide