Azaindoles as potent CRTH2 receptor antagonists

  • Bioorg Med Chem Lett. 2011 Jan 15;21(2):841-5. doi: 10.1016/j.bmcl.2010.11.084.
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
  • 1. Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Québec, Canada H9H 3L1. [email protected]
PMID: 21185722 DOI: 10.1016/j.bmcl.2010.11.084
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.