Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids
ACS Medicinal Chemistry Letters2011Vol. 2(12), pp. 938–942
Citations Over Time
Stefano Crosignani, Catherine Jorand‐Lebrun, Gordon Campbell, Adeline Prêtre, Tania Grippi-Vallotton, Anna Quattropani, Gwenaelle Bouscary‐Desforges, Agnès Bombrun, Marc Missotten, Yves Humbert, Christèle Frémaux, Mikaël Pâquet, Kamel El Harkani, Charles G. Bradshaw, Christophe Cleva, Nada Abla, Hamina Daff, Olivier Schott, Pierre-André Pittet, Jean‐François Arrighi, Marilène Gaudet, Zoë Johnson
Abstract
Antagonism of the CRTH2 receptor represents a very attractive target for a variety of allergic diseases. Most CRTH2 antagonists known to date possess a carboxylic acid moiety, which is essential for binding. However, potential acid metabolites O-acyl glucuronides might be linked to idiosynchratic toxicity in humans. In this communication, we describe a new series of compounds that lack the carboxylic acid moiety. Compounds with high affinity (Ki 1 μM). Taken together, these data show that compounds devoid of carboxylic acid groups could represent an interesting alternative to current CRTH2 antagonists in development.
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