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