Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1

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Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. / Rist, Oystein; Grimstrup, Marie; Receveur, Jean-Marie; Frimurer, Thomas M; Ulven, Trond; Kostenis, Evi; Högberg, Thomas.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 20, No. 3, 04.12.2009, p. 1177-1180.

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

Harvard

Rist, O, Grimstrup, M, Receveur, J-M, Frimurer, TM, Ulven, T, Kostenis, E & Högberg, T 2009, 'Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1', Bioorganic & Medicinal Chemistry Letters, vol. 20, no. 3, pp. 1177-1180. https://doi.org/10.1016/j.bmcl.2009.12.008

APA

Rist, O., Grimstrup, M., Receveur, J-M., Frimurer, T. M., Ulven, T., Kostenis, E., & Högberg, T. (2009). Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. Bioorganic & Medicinal Chemistry Letters, 20(3), 1177-1180. https://doi.org/10.1016/j.bmcl.2009.12.008

Vancouver

Rist O, Grimstrup M, Receveur J-M, Frimurer TM, Ulven T, Kostenis E et al. Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. Bioorganic & Medicinal Chemistry Letters. 2009 Dec 4;20(3):1177-1180. https://doi.org/10.1016/j.bmcl.2009.12.008

Author

Rist, Oystein ; Grimstrup, Marie ; Receveur, Jean-Marie ; Frimurer, Thomas M ; Ulven, Trond ; Kostenis, Evi ; Högberg, Thomas. / Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. In: Bioorganic & Medicinal Chemistry Letters. 2009 ; Vol. 20, No. 3. pp. 1177-1180.

Bibtex

@article{ba7a192dced640908775cd9ed38c8859,
title = "Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1",
abstract = "Structure-activity relationships of three related series of 4-phenylthiazol-5-ylacetic acids, derived from two hits emanating from a focused library obtained by in silico screening, have been explored as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. Several compounds with double digit nanomolar binding affinity and full antagonistic efficacy for human CRTH2 receptor were obtained in all subclasses. The most potent compound was [2-(4-chloro-benzyl)-4-(4-phenoxy-phenyl)-thiazol-5-yl]acetic acid having an binding affinity of 3.7nM and functional antagonistic effect of 66nM in a BRET and 12nM in a cAMP assay with no functional activity for the other PGD2 DP receptor (27muM in cAMP).",
author = "Oystein Rist and Marie Grimstrup and Jean-Marie Receveur and Frimurer, {Thomas M} and Trond Ulven and Evi Kostenis and Thomas H{\"o}gberg",
note = "Copyright {\textcopyright} 2009 Elsevier Ltd. All rights reserved.",
year = "2009",
month = dec,
day = "4",
doi = "10.1016/j.bmcl.2009.12.008",
language = "English",
volume = "20",
pages = "1177--1180",
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 1

AU - Rist, Oystein

AU - Grimstrup, Marie

AU - Receveur, Jean-Marie

AU - Frimurer, Thomas M

AU - Ulven, Trond

AU - Kostenis, Evi

AU - Högberg, Thomas

N1 - Copyright © 2009 Elsevier Ltd. All rights reserved.

PY - 2009/12/4

Y1 - 2009/12/4

N2 - Structure-activity relationships of three related series of 4-phenylthiazol-5-ylacetic acids, derived from two hits emanating from a focused library obtained by in silico screening, have been explored as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. Several compounds with double digit nanomolar binding affinity and full antagonistic efficacy for human CRTH2 receptor were obtained in all subclasses. The most potent compound was [2-(4-chloro-benzyl)-4-(4-phenoxy-phenyl)-thiazol-5-yl]acetic acid having an binding affinity of 3.7nM and functional antagonistic effect of 66nM in a BRET and 12nM in a cAMP assay with no functional activity for the other PGD2 DP receptor (27muM in cAMP).

AB - Structure-activity relationships of three related series of 4-phenylthiazol-5-ylacetic acids, derived from two hits emanating from a focused library obtained by in silico screening, have been explored as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells) antagonists. Several compounds with double digit nanomolar binding affinity and full antagonistic efficacy for human CRTH2 receptor were obtained in all subclasses. The most potent compound was [2-(4-chloro-benzyl)-4-(4-phenoxy-phenyl)-thiazol-5-yl]acetic acid having an binding affinity of 3.7nM and functional antagonistic effect of 66nM in a BRET and 12nM in a cAMP assay with no functional activity for the other PGD2 DP receptor (27muM in cAMP).

U2 - 10.1016/j.bmcl.2009.12.008

DO - 10.1016/j.bmcl.2009.12.008

M3 - Journal article

VL - 20

SP - 1177

EP - 1180

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 3

ER -

ID: 189159485