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ID: ALA1154943
Journal: Bioorg Med Chem Lett
Title: Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists.
Authors: Grimstrup M, Receveur JM, Rist Ø, Frimurer TM, Nielsen PA, Mathiesen JM, Högberg T.
Abstract: 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.
CiteXplore: 20137942