Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H 1 antagonists. Part II: Optimising in vivo clearance

…, R Denton, D Donald, E Kinchin, C MacDonald…

Index: Furber, Mark; Alcaraz, Lilian; Luckhurst, Christopher; Bahl, Ash; Beaton, Haydn; Bowers, Keith; Collington, John; Denton, Rebecca; Donald, David; Kinchin, Elizabeth; MacDonald, Cathy; Rigby, Aaron; Riley, Rob; Soars, Matt; Springthorpe, Brian; Webborn, Peter Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 24 p. 7707 - 7710

Full Text: HTML

Citation Number: 3

Abstract

The second part of this communication focuses on the resolution of issues surrounding the series of hydroxyamide phenoxypiperidine CCR3/H1 dual antagonists described in Part I. This involved further structural exploration directed at reducing metabolism and leading to the identification of compound 60 with a greatly improved in vivo pharmacokinetic profile.