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

M Grimstrup, Ø Rist, JM Receveur, TM Frimurer…

文献索引：Grimstrup, Marie; Rist, ystein; Receveur, Jean-Marie; Frimurer, Thomas M.; Ulven, Trond; Mathiesen, Jesper M.; Kostenis, Evi; Hoegberg, Thomas Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 1181 - 1185

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被引用次数: 10

摘要

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 ...