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

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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

Harvard

Grimstrup, M, Receveur, JM, Rist, Ø, Frimurer, TM, Nielsen, PA, Mathiesen, JM & Högberg, T 2010, 'Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 5, pp. 1638-1641. https://doi.org/10.1016/j.bmcl.2010.01.092

APA

Grimstrup, M., Receveur, J. M., Rist, Ø., Frimurer, T. M., Nielsen, P. A., Mathiesen, J. M., & Högberg, T. (2010). Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists. Bioorganic and Medicinal Chemistry Letters, 20(5), 1638-1641. https://doi.org/10.1016/j.bmcl.2010.01.092

Vancouver

Grimstrup M, Receveur JM, Rist Ø, Frimurer TM, Nielsen PA, Mathiesen JM et al. Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists. Bioorganic and Medicinal Chemistry Letters. 2010 Mar 1;20(5):1638-1641. https://doi.org/10.1016/j.bmcl.2010.01.092

Author

Grimstrup, Marie ; Receveur, Jean Marie ; Rist, Øystein ; Frimurer, Thomas M. ; Nielsen, Peter Aadal ; Mathiesen, Jesper M. ; Högberg, Thomas. / Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 5. pp. 1638-1641.

Bibtex

@article{d65d68c119014f36a6af77fb10ffefa5,

title = "Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists",

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.",

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

author = "Marie Grimstrup and Receveur, {Jean Marie} and {\O}ystein Rist and Frimurer, {Thomas M.} and Nielsen, {Peter Aadal} and Mathiesen, {Jesper M.} and Thomas H{\"o}gberg",

year = "2010",

month = mar,

day = "1",

doi = "10.1016/j.bmcl.2010.01.092",

language = "English",

volume = "20",

pages = "1638--1641",

journal = "Bioorganic & Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Pergamon Press",

number = "5",

}

RIS

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 M.

AU - Nielsen, Peter Aadal

AU - Mathiesen, Jesper M.

AU - Högberg, Thomas

PY - 2010/3/1

Y1 - 2010/3/1

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.

KW - Chemoattractant receptor-homologous molecule expressed on Th2 cells

KW - CRTH2 antagonists

KW - Molecular modelling

KW - PGD2

KW - Scaffold hopping

KW - Structure-activity relationships

UR - http://www.scopus.com/inward/record.url?scp=76649106066&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2010.01.092

DO - 10.1016/j.bmcl.2010.01.092

M3 - Journal article

C2 - 20137942

AN - SCOPUS:76649106066

VL - 20

SP - 1638

EP - 1641

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 5

ER -

ID: 221756761