Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part I

Abstract The discovery of potent small molecule dual antagonists of the human CCR3 and H 1 receptors is described for the treatment of allergic diseases, for example, asthma and allergic rhinitis. Optimizing in vitro potency and metabolic stability, starting from a CCR1 lead compound, led to compound 20 with potent dual CCR3/H 1 activity and in vitro metabolic stability.