Document Detail


2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.
MedLine Citation:
PMID:  12643939     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The structure-activity relationship of 2'-pyrrole, pyrazole and triazole substituted 2-(anilinomethyl)imidazolines as alpha(1) adrenergic agonists was investigated. The size and orientation of substituents, as well as the position of the heteroatoms, were found to have a profound effect on the potency and selectivity of the molecules. Potent alpha(1A) subtype selective agonists have been identified.
Authors:
Jason D Speake; Frank Navas; Michael J Bishop; Deanna T Garrison; Eric C Bigham; Stephen J Hodson; David L Saussy; Jim A Liacos; Paul E Irving; Bryan W Sherman
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  13     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2003 Mar 
Date Detail:
Created Date:  2003-03-19     Completed Date:  2003-10-27     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  1183-6     Citation Subset:  IM    
Affiliation:
GlaxoSmithKline, 5Moore Drive, Research Triangle Park, NC 27709, USA. jason.d.speake@gsk.com
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MeSH Terms
Descriptor/Qualifier:
Adrenergic alpha-Agonists / chemical synthesis*,  pharmacology*
Pyrazoles / chemical synthesis,  pharmacology
Pyrroles / chemical synthesis,  pharmacology
Receptors, Adrenergic, alpha-1 / agonists*
Structure-Activity Relationship
Triazoles / chemical synthesis,  pharmacology
Chemical
Reg. No./Substance:
0/Adrenergic alpha-Agonists; 0/Pyrazoles; 0/Pyrroles; 0/Receptors, Adrenergic, alpha-1; 0/Triazoles; 0/adrenergic receptor alpha(1a)

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