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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
2009-11-9
pubmed:abstractText
A series of N-(imidazolidin-2-ylidene)hydrazones and N-(4,5-dihydro-1H-imidazol-2-yl)-N-methylhydrazones were prepared and examined for alpha 1-, alpha 2-adrenergic and imidazoline I1, I2 receptors binding affinities as well as cytotoxic activity against human tumor cell lines. Among the compounds tested, 2-naphthaldehyde N-(imidazolidin-2-ylidene)hydrazone (3e) exhibited a significant affinity for both alpha 2-adrenergic and imidazoline I1 receptors (Ki = 94.3 nM and IC50 = 51.7 nM, respectively). Moreover, pyridine-2-carboxaldehyde N-(imidazolidin-2-ylidene)hydrazone (3l) showed the highest binding affinity to alpha 1-adrenoceptors (Ki = 24.6 nM), while quinoline-2-carboxaldehyde N-(imidazolidin-2-ylidene)hydrazone (3m) displayed the highest I2 affinity with a Ki value of 26.7 nM and a high selectivity with respect to alpha 2-adrenergic and imidazoline I1 receptors (Ki = 22470.0 nM and IC50 = 6145.0 nM, respectively). None of the tested N-(4,5-dihydro-1H-imidazol-2-yl)-N-methylhydrazones 4p-u displayed cytotoxic activity.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0001-6837
pubmed:author
pubmed:issnType
Print
pubmed:volume
66
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
523-34
pubmed:meshHeading
pubmed:articleTitle
Synthesis and biological activity of some 2-imidazolinylhydrazone derivatives.
pubmed:affiliation
Department of Chemical Technology of Drugs, Medical University of Gda?sk, Al. Gen. J. Hallera 107, 80-416 Gda?sk, Poland. a.kornicka@amg.gda.pl
pubmed:publicationType
Journal Article