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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
|
pubmed:dateCreated |
1992-4-3
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pubmed:abstractText |
As part of a program aimed at identifying novel analogues of diltiazem, we developed several synthetic routes for 3-alkylbenzazepinones, both in racemic and nonracemic form. Structure-activity relationship studies in this series have led to identification of several analogues as potent calcium channel blocking agents, both in vitro and in vivo. Analogues containing a 6-trifluoromethyl substituent (17a and 17b) are the most potent vasorelaxants in vitro. The oral antihypertensive activity of these compounds is comparable to its 3-acetoxy derivative 1 (X = 6-CF3) and 8-chlorodiltiazem (2b). The 3-allyl analogue 17c is a more potent antihypertensive agent than 17a, 17b, or 8-chlorodiltiazem (2b), and has a longer duration of action in vivo.
|
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Feb
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
21
|
pubmed:volume |
35
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
N
|
pubmed:pagination |
773-80
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1542103-Animals,
pubmed-meshheading:1542103-Antihypertensive Agents,
pubmed-meshheading:1542103-Aorta,
pubmed-meshheading:1542103-Benzazepines,
pubmed-meshheading:1542103-Calcium Channel Blockers,
pubmed-meshheading:1542103-Guinea Pigs,
pubmed-meshheading:1542103-Hypertension,
pubmed-meshheading:1542103-Male,
pubmed-meshheading:1542103-Molecular Conformation,
pubmed-meshheading:1542103-Molecular Structure,
pubmed-meshheading:1542103-Muscles,
pubmed-meshheading:1542103-Rabbits,
pubmed-meshheading:1542103-Rats,
pubmed-meshheading:1542103-Rats, Inbred SHR,
pubmed-meshheading:1542103-Structure-Activity Relationship,
pubmed-meshheading:1542103-Vasodilation,
pubmed-meshheading:1542103-X-Ray Diffraction
|
pubmed:year |
1992
|
pubmed:articleTitle |
Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones.
|
pubmed:affiliation |
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543-4000.
|
pubmed:publicationType |
Journal Article,
Comparative Study
|