CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure–activity relationships

Abstract CCR3 antagonist leads with IC 50 values in the μM range were converted into low nM binding compounds that displayed in vitro inhibition of human eosinophil chemotaxis induced by human eotaxin. In particular, 4-benzylpiperidin-1-yl- n -propylureas and erythro -3-(4-benzyl-2-(α-hydroxyalkyl)piperidin-1-yl)- n -propylureas (obtained via Beak reaction of N -BOC-4-benzylpiperidine) exhibited single digit nanomolar IC 50 values for CCR3.