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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1996-3-1
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pubmed:abstractText |
A series of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds were prepared and evaluated for their antagonistic activities to the angiotensin II (AII) receptor. Among them, the 4-(1-hydroxyalkyl)-imidazole derivatives had strong binding affinity to the AII receptor and potently inhibited the AII-induced pressor response by intravenous administration. Various esters of these acids showed potent and long-lasting antagonistic activity by oral administration. The most promising compounds were (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (CS-866) and (pivaloyloxy)-methyl esters of 4-(1-hydroxy-1-methylethyl)-2-propyl-1-[(2'-1H-tetrazol-5- ylbiphenyl-4-yl)-methyl]imidazole-5-carboxylic acid (26c). A study involving stereochemical comparison of 26c with the acetylated C-terminal pentapeptide of AII was also undertaken.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AmemiyaYY,
pubmed-author:FujimotoKK,
pubmed-author:FurukawaYY,
pubmed-author:IkedaMM,
pubmed-author:KanazakiTT,
pubmed-author:KitaharaYY,
pubmed-author:KoikeHH,
pubmed-author:MiyamotoSS,
pubmed-author:MizunoMM,
pubmed-author:SadaTT,
pubmed-author:ShimojiYY,
pubmed-author:YanagisawaHH
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pubmed:issnType |
Print
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pubmed:day |
5
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pubmed:volume |
39
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
323-38
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:8568823-Acetylation,
pubmed-meshheading:8568823-Adrenal Cortex,
pubmed-meshheading:8568823-Amino Acid Sequence,
pubmed-meshheading:8568823-Angiotensin II,
pubmed-meshheading:8568823-Angiotensin Receptor Antagonists,
pubmed-meshheading:8568823-Animals,
pubmed-meshheading:8568823-Antihypertensive Agents,
pubmed-meshheading:8568823-Biological Availability,
pubmed-meshheading:8568823-Cattle,
pubmed-meshheading:8568823-Imidazoles,
pubmed-meshheading:8568823-Kinetics,
pubmed-meshheading:8568823-Male,
pubmed-meshheading:8568823-Models, Molecular,
pubmed-meshheading:8568823-Molecular Conformation,
pubmed-meshheading:8568823-Molecular Sequence Data,
pubmed-meshheading:8568823-Molecular Structure,
pubmed-meshheading:8568823-Rats,
pubmed-meshheading:8568823-Rats, Wistar,
pubmed-meshheading:8568823-Receptors, Angiotensin,
pubmed-meshheading:8568823-Structure-Activity Relationship
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pubmed:year |
1996
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pubmed:articleTitle |
Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds.
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pubmed:affiliation |
Research Institute, Sankyo Company, Ltd., Tokyo, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro
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