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

Authors :
Bahl A
Barton P
Bowers K
Brough S
Evans R
Luckhurst CA
Mochel T
Perry MW
Rigby A
Riley RJ
Sanganee H
Sisson A
Springthorpe B
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Nov 01; Vol. 22 (21), pp. 6688-93. Date of Electronic Publication: 2012 Sep 15.
Publication Year :
2012

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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
22
Issue :
21
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
23031591
Full Text :
https://doi.org/10.1016/j.bmcl.2012.08.124