Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2

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Standard

Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. / Grimstrup, Marie; Rist, Øystein; Receveur, Jean-Marie; Frimurer, Thomas M; Ulven, Trond; Mathiesen, Jesper M; Kostenis, Evi; Högberg, Thomas.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 20, No. 3, 01.02.2010, p. 1181-1185.

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

Harvard

Grimstrup, M, Rist, Ø, Receveur, J-M, Frimurer, TM, Ulven, T, Mathiesen, JM, Kostenis, E & Högberg, T 2010, 'Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2', Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 3, pp. 1181-1185. https://doi.org/10.1016/j.bmcl.2009.12.015

APA

Grimstrup, M., Rist, Ø., Receveur, J-M., Frimurer, T. M., Ulven, T., Mathiesen, J. M., Kostenis, E., & Högberg, T. (2010). Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. Bioorganic & Medicinal Chemistry Letters, 20(3), 1181-1185. https://doi.org/10.1016/j.bmcl.2009.12.015

Vancouver

Grimstrup M, Rist Ø, Receveur J-M, Frimurer TM, Ulven T, Mathiesen JM et al. Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. Bioorganic & Medicinal Chemistry Letters. 2010 Feb 1;20(3):1181-1185. https://doi.org/10.1016/j.bmcl.2009.12.015

Author

Grimstrup, Marie ; Rist, Øystein ; Receveur, Jean-Marie ; Frimurer, Thomas M ; Ulven, Trond ; Mathiesen, Jesper M ; Kostenis, Evi ; Högberg, Thomas. / Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. In: Bioorganic & Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 3. pp. 1181-1185.

Bibtex

@article{63c2d83fd966478a82856669f4ce5ca4,
title = "Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2",
abstract = "Structure-activity relationships have been established by exploring the eastern and western side of 5-thiazolyleacetic acids as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. Benzhydryl motifs in the 2-position of the thiazole was found to be most advantageous. The 4-thiazole position should either carry 3- or 4-fluorophenyl rings or a 4-pyridyl suitably substituted in the flanking 2-position. Several compounds with single digit nanomolar binding affinity and full antagonistic efficacy for human CRTH2 receptor were obtained. The compound series display a good PK profile and selectivity over a large number of other targets.",
author = "Marie Grimstrup and {\O}ystein Rist and Jean-Marie Receveur and Frimurer, {Thomas M} and Trond Ulven and Mathiesen, {Jesper M} and Evi Kostenis and Thomas H{\"o}gberg",
note = "Copyright (c) 2009 Elsevier Ltd. All rights reserved.",
year = "2010",
month = feb,
day = "1",
doi = "10.1016/j.bmcl.2009.12.015",
language = "English",
volume = "20",
pages = "1181--1185",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Pergamon Press",
number = "3",

}

RIS

TY - JOUR

T1 - Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2

AU - Grimstrup, Marie

AU - Rist, Øystein

AU - Receveur, Jean-Marie

AU - Frimurer, Thomas M

AU - Ulven, Trond

AU - Mathiesen, Jesper M

AU - Kostenis, Evi

AU - Högberg, Thomas

N1 - Copyright (c) 2009 Elsevier Ltd. All rights reserved.

PY - 2010/2/1

Y1 - 2010/2/1

N2 - Structure-activity relationships have been established by exploring the eastern and western side of 5-thiazolyleacetic acids as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. Benzhydryl motifs in the 2-position of the thiazole was found to be most advantageous. The 4-thiazole position should either carry 3- or 4-fluorophenyl rings or a 4-pyridyl suitably substituted in the flanking 2-position. Several compounds with single digit nanomolar binding affinity and full antagonistic efficacy for human CRTH2 receptor were obtained. The compound series display a good PK profile and selectivity over a large number of other targets.

AB - Structure-activity relationships have been established by exploring the eastern and western side of 5-thiazolyleacetic acids as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. Benzhydryl motifs in the 2-position of the thiazole was found to be most advantageous. The 4-thiazole position should either carry 3- or 4-fluorophenyl rings or a 4-pyridyl suitably substituted in the flanking 2-position. Several compounds with single digit nanomolar binding affinity and full antagonistic efficacy for human CRTH2 receptor were obtained. The compound series display a good PK profile and selectivity over a large number of other targets.

U2 - 10.1016/j.bmcl.2009.12.015

DO - 10.1016/j.bmcl.2009.12.015

M3 - Journal article

VL - 20

SP - 1181

EP - 1185

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 3

ER -

ID: 189161819