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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1989-3-8
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pubmed:abstractText |
(4S)-1-Alkyl-3-[[N-(carboxyalkyl)amino]acyl]-2-oxoimidazolidine-4- carboxylic acid derivatives (3) were prepared by two methods. Their angiotensin converting enzyme (ACE) inhibitory activities and antihypertensive effects were evaluated, and the structure-activity relationships were discussed. The dicarboxylic acids 3a-n possessing S,S,S configuration showed potent in vitro ACE inhibitory activities with IC50 values of 1.1 X 10(-8)-1.5 X 10(-9) M. The most potent compound in this series, monoester 3p, had an ID50 value of 0.24 mg/kg, po for inhibition of angiotensin I induced pressor response in normotensive rats and produced a dose-dependent decrease in systolic blood pressure of spontaneously hypertensive rats (SHRs) at doses of 1-10 mg/kg, po.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
32
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
289-97
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:2913292-Angiotensin-Converting Enzyme Inhibitors,
pubmed-meshheading:2913292-Animals,
pubmed-meshheading:2913292-Blood Pressure,
pubmed-meshheading:2913292-Carboxylic Acids,
pubmed-meshheading:2913292-Imidazoles,
pubmed-meshheading:2913292-Male,
pubmed-meshheading:2913292-Rats,
pubmed-meshheading:2913292-Rats, Inbred SHR,
pubmed-meshheading:2913292-Rats, Inbred Strains,
pubmed-meshheading:2913292-Structure-Activity Relationship
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pubmed:year |
1989
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pubmed:articleTitle |
Studies on angiotensin converting enzyme inhibitors. 4. Synthesis and angiotensin converting enzyme inhibitory activities of 3-acyl-1-alkyl-2-oxoimidazolidine-4-carboxylic acid derivatives.
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pubmed:affiliation |
Research Laboratory of Applied Biochemistry and Safety Research Laboratory, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
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pubmed:publicationType |
Journal Article
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