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. 2011 Jan 15;21(2):841-5.
doi: 10.1016/j.bmcl.2010.11.084. Epub 2010 Nov 21.

Azaindoles as potent CRTH2 receptor antagonists

Daniel Simard  1 , Yves Leblanc, Carl Berthelette, M Helmi Zaghdane, Carmela Molinaro, Zhaoyin Wang, Michel Gallant, Stephen Lau, Trinh Thao, Martine Hamel, Rino Stocco, Nicole Sawyer, Susan Sillaots, Francois Gervais, Robert Houle, Jean-François Lévesque
Affiliations

Azaindoles as potent CRTH2 receptor antagonists

Daniel Simard et al. Bioorg Med Chem Lett. .

Abstract

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.

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