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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
1992-5-12
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pubmed:abstractText |
A series of pyrimido[1,2-a]indoles were synthesized and studied for their hypoglycemic activity following oral administration at a standard dose of 100 mg/kg to fed rats. The effect of 10-alkoxyalkyl, 10-alkyl, 10-aryl, and 3,3-dialkyl substitution on the activity of 10-hydroxypyrimido[1,2-a]indoles was investigated. Relative potencies of a number of the most active compounds were defined by three-point dose-response studies. The most potent compounds were those with either 3,3-dimethyl substituents, compounds 21, 22, and 38, or 3,3-spirocyclohexane substituents, compounds 39 and 49. 10-Aminopyrimido[1,2-a]indoles were in general less active than the 10-hydroxy analogues, and potency was further decreased by derivatizing the 10-amino group. The most potent 10-amino derivatives were 57 and 58.
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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/Blood Glucose,
http://linkedlifedata.com/resource/pubmed/chemical/Hypoglycemic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrimidines,
http://linkedlifedata.com/resource/pubmed/chemical/ciclazindol
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
3
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pubmed:volume |
35
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
1169-75
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1560431-Animals,
pubmed-meshheading:1560431-Blood Glucose,
pubmed-meshheading:1560431-Dose-Response Relationship, Drug,
pubmed-meshheading:1560431-Hypoglycemic Agents,
pubmed-meshheading:1560431-Indoles,
pubmed-meshheading:1560431-Male,
pubmed-meshheading:1560431-Molecular Structure,
pubmed-meshheading:1560431-Pyrimidines,
pubmed-meshheading:1560431-Rats,
pubmed-meshheading:1560431-Rats, Inbred Strains,
pubmed-meshheading:1560431-Structure-Activity Relationship
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pubmed:year |
1992
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pubmed:articleTitle |
Oral hypoglycemic agents. Pyrimido[1,2-a]indoles and related compounds.
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pubmed:affiliation |
Department of Medicinal Chemistry, Wyeth Research, Maidenhead, Berkshire, England.
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pubmed:publicationType |
Journal Article,
Comparative Study
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