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Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part II: Optimising in vivo clearance |
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| Authors: | Mark Furber Lilian Alcaraz Christopher Luckhurst Ash Bahl Haydn Beaton Keith Bowers John Collington Rebecca Denton David Donald Elizabeth Kinchin Cathy MacDonald Aaron Rigby Rob Riley Matt Soars Brian Springthorpe Peter Webborn |
| Affiliation: | 1. Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, Leicestershire, LE11 5RH, UK;2. Discovery Biosciences, AstraZeneca R&D Charnwood, Loughborough, Leicestershire, LE11 5RH, UK;3. Physical and Metabolic Sciences, AstraZeneca R&D Charnwood, Loughborough, Leicestershire, LE11 5RH, UK;4. AstraZeneca Respiratory & Inflammation iMED, Pepparedsleden 1, 431 83 Mölndal, Sweden |
| 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. |
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