Document Detail


Indole 5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase with nanomolar potency in cell-based subgenomic replicons (part 2): Central amino acid linker and right-hand-side SAR studies.
MedLine Citation:
PMID:  21592789     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
In this part 2, new indole 5-carboxamide Thumb Pocket 1 inhibitors of HCV NS5B polymerase are described. Structure-activity relationships (SAR) were explored at the central amino acid linker position and the right-hand-side of the molecule in an attempt to identify molecules with a balanced overall profile of potency (EC(50)<100nM), physicochemical properties and ADME characteristics.
Authors:
Pierre L Beaulieu; Catherine Chabot; Jianmin Duan; Michel Garneau; James Gillard; Eric Jolicoeur; Martin Poirier; Marc-André Poupart; Timothy A Stammers; George Kukolj; Youla S Tsantrizos
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-4-24
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2011 Apr 
Date Detail:
Created Date:  2011-5-19     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 © 2011 Elsevier Ltd. All rights reserved.
Affiliation:
Department of Chemistry, Boehringer Ingelheim (Canada) Ltd, Research and Development, 2100 Cunard Street, Laval (Québec), Canada H7S 2G5.
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