1220098-03-2Relevant articles and documents
Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists
Grimstrup, Marie,Receveur, Jean-Marie,Rist, ?ystein,Frimurer, Thomas M.,Nielsen, Peter Aadal,Mathiesen, Jesper M.,H?gberg, Thomas
scheme or table, p. 1638 - 1641 (2010/07/15)
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.
