Azaindoles as potent CRTH2 receptor antagonists

…, MH Zaghdane, C Molinaro, Z Wang, M Gallant…

文献索引：Simard, Daniel; Leblanc, Yves; Berthelette, Carl; Zaghdane, M. Helmi; Molinaro, Carmela; Wang, Zhaoyin; Gallant, Michel; Lau, Stephen; Thao, Trinh; Hamel, Martine; Stocco, Rino; Sawyer, Nicole; Sillaots, Susan; Gervais, Francois; Houle, Robert; Levesque, Jean-Franois Bioorganic and Medicinal Chemistry Letters, 2011 ,  vol. 21,  # 2  p. 841 - 845

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被引用次数: 16

摘要

A new class of 7-azaindole analogs of MK-7246 as potent and selective CRTH2 antagonists is reported. The SAR leading to the identification of the optimal azaindole regioisomer as well as the pharmacokinetics and off-target activities of the most potent antagonists are disclosed.