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Bioorg Med Chem Lett. 2012 Nov 1;22(21):6688-93. doi: 10.1016/j.bmcl.2012.08.124. Epub 2012 Sep 15.

The discovery of CCR3/H1 dual antagonists with reduced hERG risk.

Author information

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

Abstract

A series of dual CCR3/H(1) antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to deliver a compound suitable for clinical evaluation.

PMID:
23031591
DOI:
10.1016/j.bmcl.2012.08.124
[Indexed for MEDLINE]

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