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.
Original language | English |
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Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 20 |
Issue number | 5 |
Pages (from-to) | 1638-1641 |
Number of pages | 4 |
ISSN | 0960-894X |
DOIs | |
Publication status | Published - 1 Mar 2010 |
- Chemoattractant receptor-homologous molecule expressed on Th2 cells, CRTH2 antagonists, Molecular modelling, PGD2, Scaffold hopping, Structure-activity relationships
Research areas
ID: 221756761