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Bioorg Med Chem Lett. 2012 Nov 1;22(21):6694-9. doi: 10.1016/j.bmcl.2012.08.103. Epub 2012 Sep 11.

Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092.

Author information

1
Department of Bioscience, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, United Kingdom.

Abstract

The discovery and optimisation of a series of zwitterionic CCR3 antagonists is described. Optimisation of the structure led to AZ12436092, a compound with excellent selectivity over activity at hERG and outstanding pharmacokinetics in preclinical species.

PMID:
23021991
DOI:
10.1016/j.bmcl.2012.08.103
[Indexed for MEDLINE]

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