Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists
Research output: Contribution to journal › Journal article › Research › peer-review
The SAR features have been further explored for (2-benzhydryl-4-phenyl-thiazol-5-yl)acetic acids as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. The introduction of a nitrogen or a methyl substituent in the benzhydrylic position offer two alternative drugable scaffolds attractive for unsymmetrically substituted derivatives. An imidazole analogue lacks activity due to formation of a favored coplanar intramolecular hydrogen bond. The pyrimidine derivative 18 represents a potent and selective compound that will be subject to continued investigations.
|Journal||Bioorganic and Medicinal Chemistry Letters|
|Number of pages||4|
|Publication status||Published - 1 Mar 2010|
- Chemoattractant receptor-homologous molecule expressed on Th2 cells, CRTH2 antagonists, Molecular modelling, PGD2, Scaffold hopping, Structure-activity relationships