2. Academic Validation
  3. Azaindoles as potent CRTH2 receptor antagonists

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

Affiliation

  • 1 Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Québec, Canada H9H 3L1. daniel.simard@merck.com
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.

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