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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
1993-6-22
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pubmed:abstractText |
Several heterocyclic analogues of the potent 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines were synthesized and evaluated for their antagonistic calcium activities in comparison with the 1-sulfonylindolizine SR 33557 and the usual calcium antagonist references verapamil, cis-(+)-diltiazem, and nifedipine. The bicyclic nine-membered rings were, in general, more potent than the bicyclic 10-membered or five-membered rings. Among the bicyclic nine-membered rings, the indole nucleus appeared to be extremely favorable to support the calcium antagonistic activity. In particular, compound 36, with an IC50 value for the inhibition of [3H]nitrendipine equal to 0.072 nM, is among the most potent calcium antagonist known. This compound has been selected for clinical development.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Heterocyclic Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Indolizines,
http://linkedlifedata.com/resource/pubmed/chemical/Phenethylamines,
http://linkedlifedata.com/resource/pubmed/chemical/fantofarone
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
36
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pubmed:owner |
NLM
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pubmed:authorsComplete |
N
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pubmed:pagination |
1425-33
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8496910-Animals,
pubmed-meshheading:8496910-Calcium Channel Blockers,
pubmed-meshheading:8496910-Cerebral Cortex,
pubmed-meshheading:8496910-Guinea Pigs,
pubmed-meshheading:8496910-Heterocyclic Compounds,
pubmed-meshheading:8496910-Indolizines,
pubmed-meshheading:8496910-Male,
pubmed-meshheading:8496910-Muscle, Smooth, Vascular,
pubmed-meshheading:8496910-Phenethylamines,
pubmed-meshheading:8496910-Rats,
pubmed-meshheading:8496910-Rats, Wistar,
pubmed-meshheading:8496910-Structure-Activity Relationship
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pubmed:year |
1993
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pubmed:articleTitle |
Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
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pubmed:affiliation |
Sanofi Research Center, Brussels, Belgium.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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