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

Marie Grimstrup; Jean Marie Receveur; Øystein Rist; Thomas M. Frimurer; Peter Aadal Nielsen; Jesper M. Mathiesen; Thomas Högberg

doi:10.1016/j.bmcl.2010.01.092

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

Marie Grimstrup, Jean Marie Receveur, Øystein Rist, Thomas M. Frimurer, Peter Aadal Nielsen, Jesper M. Mathiesen, Thomas Högberg^*

^*Corresponding author for this work

Research output: Contribution to journal › Journal article › Research › peer-review

16 Citations (Scopus)

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.

Original language	English
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	5
Pages (from-to)	1638-1641
Number of pages	4
ISSN	0960-894X
DOIs	https://doi.org/10.1016/j.bmcl.2010.01.092
Publication status	Published - 1 Mar 2010

Keywords

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

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10.1016/j.bmcl.2010.01.092

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Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists. / Grimstrup, Marie; Receveur, Jean Marie; Rist, Øystein; Frimurer, Thomas M.; Nielsen, Peter Aadal; Mathiesen, Jesper M.; Högberg, Thomas.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 5, 01.03.2010, p. 1638-1641.

Research output: Contribution to journal › Journal article › Research › peer-review

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AU - Högberg, Thomas

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

Abstract

Keywords

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