Abstract
Hits from an in silico derived focused library for CRTH2 were transformed into highly selective antagonists with favorable ADME properties. Oral administration of 4-bromo-2-(1-phenyl-1H-pyrazole-4-carbonyl)phenoxyacetic acid (19) inhibited peribronchial eosinophilia and mucus cell hyperplasia in a mouse model of allergic asthma, supporting the therapeutic potential of this novel compound class. In addition, this selective pharmacological tool compound provides further evidence for CRTH2 as a relevant therapeutic target for treatment of Th2- and eosinophil-related inflammation.
Original language | English |
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Pages (from-to) | 6638-6641 |
Journal | Journal of Medicinal Chemistry |
Volume | 49 |
Issue number | 23 |
DOIs | |
Publication status | Published - 2006 |
Subject classification (UKÄ)
- Cell and Molecular Biology