Ontology highlight
ABSTRACT:
SUBMITTER: Crosignani S
PROVIDER: S-EPMC4018148 | biostudies-literature | 2011 Dec
REPOSITORIES: biostudies-literature
Crosignani Stefano S Jorand-Lebrun Catherine C Campbell Gordon G Prêtre Adeline A Grippi-Vallotton Tania T Quattropani Anna A Bouscary-Desforges Gwenaelle G Bombrun Agnes A Missotten Marc M Humbert Yves Y Frémaux Christèle C Pâquet Mikaël M El Harkani Kamel K Bradshaw Charles G CG Cleva Christophe C Abla Nada N Daff Hamina H Schott Olivier O Pittet Pierre-André PA Arrighi Jean-François JF Gaudet Marilène M Johnson Zoë Z
ACS medicinal chemistry letters 20111010 12
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 (K i < 10 nM) for the receptor have been identified. S ...[more]