@article{1dc89f2018a211dfba21000ea68e967b,
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--5",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier",
number = "3",
}