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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7707-10. doi: 10.1016/j.bmcl.2012.09.112. Epub 2012 Oct 10.

Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H₁ antagonists. Part II: optimising in vivo clearance.

Author information

1
AstraZeneca Respiratory & Inflammation iMED, Pepparedsleden 1, 431 83 Mölndal, Sweden. mark1.furber@astrazeneca.com

Abstract

The second part of this communication focuses on the resolution of issues surrounding the series of hydroxyamide phenoxypiperidine CCR3/H(1) 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.

PMID:
23116889
DOI:
10.1016/j.bmcl.2012.09.112
[Indexed for MEDLINE]

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