Document Detail


Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs).
MedLine Citation:
PMID:  19846298     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
A variety of basic, heterocyclic templates has been reported as potassium-competitive, acid pump antagonists. Herein, we report a comparison of potencies of these templates and others to establish which offers the best start point for further systematic optimisation. Modifications were carried out to improve the developability profile of the more potent 1H-pyrrolo[2,3-c]pyridine template, affording molecules with improved overall in vitro characteristics versus the reported clinical candidate AR-H047108, and comparable to the clinically efficacious AZD-0865.
Authors:
Terry Panchal; Nick Bailey; Mark Bamford; Emmanuel Demont; Richard Elliott; Irene Farre-Gutierrez; Neil Garton; Thomas Hayhow; Gail Hutley; Antoinette Naylor
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Publication Detail:
Type:  Journal Article     Date:  2009-07-04
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  19     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2009 Dec 
Date Detail:
Created Date:  2009-11-05     Completed Date:  2010-01-19     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  6813-7     Citation Subset:  IM    
Affiliation:
Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline R&D, Harlow, Essex CM19 5AW, United Kingdom. Terry.A.Panchal@gsk.com
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MeSH Terms
Descriptor/Qualifier:
Binding, Competitive
Drug Design
H(+)-K(+)-Exchanging ATPase / antagonists & inhibitors*
Heterocyclic Compounds / chemical synthesis,  chemistry,  pharmacology*
Molecular Structure
Pyridines / chemical synthesis,  chemistry,  pharmacology*
Stereoisomerism
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Heterocyclic Compounds; 0/Pyridines; EC 3.6.1.10/H(+)-K(+)-Exchanging ATPase

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


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