Preparation of the I-3 imidazoline receptor antagonist KU14R and related 2,3-dihydrobenzo[b]furan derivatives

The preparation and characterisation of a series of novel analogues of the imidazoline insulin secretagogue efaroxan, including the I-3-receptor antagonist KU14R, are described. Replacement of the imidazoline ring of efaroxan by selected functional groups leads either to loss of activity or to very...

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Bibliographic Details
Published inSynthesis (Stuttgart) no. 10; pp. 1546 - 1550
Main Authors Clews, J, Morgan, NG, Ramsden, CA
Format Journal Article
LanguageEnglish
Published STUTTGART Thieme Medical Publishers 01.08.2001
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
REAGENTS
imidazole
tetrazole
insulin
RAT
ISLETS
INSULIN-SECRETION
I-3-receptor
antagonist
SITES
efaroxan
LIGAND
imidazoline
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Summary:The preparation and characterisation of a series of novel analogues of the imidazoline insulin secretagogue efaroxan, including the I-3-receptor antagonist KU14R, are described. Replacement of the imidazoline ring of efaroxan by selected functional groups leads either to loss of activity or to very weak I-3-agonist activity in insulin secretion studies. The imidazole analogue KU14R was found to be an I-3-antagonist in this assay and useful as a biological tool.
ISSN:0039-7881
DOI:10.1055/s-2001-16079