TY - JOUR
T1 - Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists
AU - Grimstrup, Marie
AU - Receveur, Jean-Marie
AU - Rist, Øystein
AU - Frimurer, Thomas
AU - Nielsen, Peter Aadal
AU - Mathiesen, Jesper M.
AU - Högberg, Thomas
N1 - Copyright 2010 Elsevier Ltd. All rights reserved.
PY - 2010
Y1 - 2010
N2 - 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.
AB - 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.
U2 - 10.1016/j.bmcl.2010.01.092
DO - 10.1016/j.bmcl.2010.01.092
M3 - Journal article
C2 - 20137942
SN - 0960-894X
VL - 20
SP - 1638
EP - 1641
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
IS - 5
ER -