Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists

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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 languageEnglish
JournalBioorganic and Medicinal Chemistry Letters
Issue number5
Pages (from-to)1638-1641
Number of pages4
Publication statusPublished - 1 Mar 2010

    Research areas

  • Chemoattractant receptor-homologous molecule expressed on Th2 cells, CRTH2 antagonists, Molecular modelling, PGD2, Scaffold hopping, Structure-activity relationships

ID: 221756761