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

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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.
Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Issue number3
Pages (from-to)1181-1185
Number of pages5
Publication statusPublished - 1 Feb 2010

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