| 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...