Referenced in: none

Automatically associated channels: Kv11.1

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

Authors: Ash Bahl, Patrick Barton, Keith Bowers, Steven Brough, Richard Evans, Christopher A Luckhurst, Tobias Mochel, Matthew W D Perry, Aaron Rigby, Robert J Riley, Hitesh Sanganee, Adam Sisson, Brian Springthorpe

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 Nov 1 , 22, 6688-93

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23031591

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.