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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
1998-11-23
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pubmed:abstractText |
Described in this paper is the synthesis and pharmacological activity of five metabolites of the angiotensin II antagonist tasosartan (1). Of particular interest is the effect of the additional acidic group of the enol metabolite (8) on activity. As suggested by the structural-activity relationship of other angiotensin II antagonist series, a second acidic group can improve receptor binding activity but decrease in vivo activity after oral dosing. The metabolic introduction of a second acidic group in tasosartan bypasses this problem and contributes to the excellent profile of the compound. A molecular modeling study provides a rationale for the role of the enol group of 8 in AT1 receptor binding.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Angiotensin II,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridones,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Angiotensin, Type 1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Angiotensin, Type 2,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Angiotensin,
http://linkedlifedata.com/resource/pubmed/chemical/Tetrazoles,
http://linkedlifedata.com/resource/pubmed/chemical/tasosartan
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AntaneMM,
pubmed-author:BagliJ FJF,
pubmed-author:ChenJJ,
pubmed-author:ColliniM DMD,
pubmed-author:EllingboeJ WJW,
pubmed-author:HartupeeDD,
pubmed-author:ParkC HCH,
pubmed-author:QuagliatoDD,
pubmed-author:SchmidJJ,
pubmed-author:TanikellaTT,
pubmed-author:WhiteVV
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pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
41
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4251-60
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:9784100-Administration, Oral,
pubmed-meshheading:9784100-Adrenal Glands,
pubmed-meshheading:9784100-Angiotensin II,
pubmed-meshheading:9784100-Animals,
pubmed-meshheading:9784100-Blood Pressure,
pubmed-meshheading:9784100-Heart Rate,
pubmed-meshheading:9784100-Hypertension,
pubmed-meshheading:9784100-Injections, Intravenous,
pubmed-meshheading:9784100-Liver,
pubmed-meshheading:9784100-Models, Molecular,
pubmed-meshheading:9784100-Molecular Conformation,
pubmed-meshheading:9784100-Pyridones,
pubmed-meshheading:9784100-Pyrimidines,
pubmed-meshheading:9784100-Rats,
pubmed-meshheading:9784100-Rats, Sprague-Dawley,
pubmed-meshheading:9784100-Receptor, Angiotensin, Type 1,
pubmed-meshheading:9784100-Receptor, Angiotensin, Type 2,
pubmed-meshheading:9784100-Receptors, Angiotensin,
pubmed-meshheading:9784100-Structure-Activity Relationship,
pubmed-meshheading:9784100-Tetrazoles
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pubmed:year |
1998
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pubmed:articleTitle |
Metabolites of the angiotensin II antagonist tasosartan: the importance of a second acidic group.
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pubmed:affiliation |
Divisions of Chemical Sciences, Cardiovascular and Metabolic Disorders, and Structural Biology, Wyeth-Ayerst Research, CN 8000, Princeton, New Jersey 08543, USA.
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pubmed:publicationType |
Journal Article,
In Vitro
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