Document Detail


The discovery of CCR3/H(1) dual antagonists with reduced hERG risk.
MedLine Citation:
PMID:  23031591     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
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
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-9-15
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2012 Sep 
Date Detail:
Created Date:  2012-10-3     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 Elsevier Ltd. All rights reserved.
Affiliation:
Department of Bioscience, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, United Kingdom.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  Identification of a glutathione peroxidase inhibitor that reverses resistance to anticancer drugs in...
Next Document:  Downregulation of mdr1 and abcg2 genes is a mechanism of inhibition of efflux pumps mediated by poly...