Linked Life Data

2342074

Source:http://linkedlifedata.com/resource/pubmed/id/2342074

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1990-6-28
pubmed:abstractText
The synthesis of a series of 1,4-dihydropyridines which have N-linked heterocycles at the terminus of an ethoxymethyl chain at the 2-position is described. The calcium antagonist activity on rat aorta of this class of DHPs is compared with their negative inotropic activity as determined by using a Langendorff-perfused guinea pig heart model. The compounds examined show a wide range of selectivity for vascular over cardiac tissue, with those analogues which possess an amide group at the terminus of the 2-substituent proving the most selective. From the in vitro data obtained for a series of 1,2,3-triazoles, it is possible to conclude that the SARs for binding to the calcium channels in vascular and cardiac tissue are different. One of the compounds, 2-amino-1-[2-[[4-(2,3-dichlorophenyl)-3-(ethoxycarbonyl)-5- (methoxycarbonyl)-6-methyl-1,4-dihydropyrid-2-yl]methoxy]ethyl]-4( 3H)- imidazolone (20b, UK-55,444), was identified as a potent (IC50 = 8 x 10(-9) M) calcium antagonist which is 40-fold selective for vascular over cardiac tissue and which has a significantly longer duration of action (greater than 3 h) than nifedipine in the anesthetized dog on intravenous administration.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
33
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1805-11
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1990
pubmed:articleTitle
Long-acting dihydropyridine calcium antagonists. 5. Synthesis and structure-activity relationships for a series of 2-[[(N-substituted-heterocyclyl)ethoxy]methyl]-1,4-dihydropyridine calcium antagonists.
pubmed:affiliation
Pfizer Central Research, Sandwich, Kent, United Kingdom.
pubmed:publicationType
Journal Article, In Vitro