Document Detail


Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.
MedLine Citation:
PMID:  20171098     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Three novel series of histamine H(4) receptor (H(4)R) antagonists containing the 2-aminopyrimidine motif are reported. The best of these compounds display good in vitro potency in both functional and binding assays. In addition, representative compounds are able to completely block itch responses when dosed ip in a mouse model of H(4)-agonist induced scratching, thus demonstrating their activities as H(4)R antagonists.
Authors:
John R Koenig; Huaqing Liu; Irene Drizin; David G Witte; Tracy L Carr; Arlene M Manelli; Ivan Milicic; Marina I Strakhova; Thomas R Miller; Timothy A Esbenshade; Jorge D Brioni; Marlon Cowart
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Publication Detail:
Type:  Journal Article     Date:  2010-02-01
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Mar 
Date Detail:
Created Date:  2010-03-08     Completed Date:  2010-07-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  1900-4     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier Ltd. All rights reserved.
Affiliation:
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6100, USA. john.r.koenig@abbott.com
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MeSH Terms
Descriptor/Qualifier:
Aminopyridines / pharmacology*
Animals
Histamine Antagonists / pharmacology*
Humans
Mice
Receptors, G-Protein-Coupled / antagonists & inhibitors*
Receptors, Histamine
Chemical
Reg. No./Substance:
0/Aminopyridines; 0/Histamine Antagonists; 0/Hrh4 protein, mouse; 0/Receptors, G-Protein-Coupled; 0/Receptors, Histamine; 504-29-0/alpha-aminopyridine

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