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1-(2,6-Diisopropylphenyl)-3-(1,3-dimethyl-2,6-dioxo-2,3,6,7- tetrahydro-1H-purin-8/7-ylalkyl)ureas as Potential Acyl-CoA: Cholesterol Acyltransferase Inhibitors
Rybár, A., Alföldi, J., Faberová, V. and Schmidtová, Ľ. 1-(2,6-Diisopropylphenyl)-3-(1,3-dimethyl-2,6-dioxo-2,3,6,7- tetrahydro-1H-purin-8/7-ylalkyl)ureas as Potential Acyl-CoA: Cholesterol Acyltransferase Inhibitors Chemical Papers, Vol.56, No. 5, 2002, 330-339
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Document type:
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Článok z časopisu / Journal Article |
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Collection:
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Chemical papers
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| Attached Files |
| Name |
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MIMEType |
Size |
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n565a330.pdf
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565a330.pdf |
application/pdf |
222.04KB |
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| Author(s) |
Rybár, A.
Alföldi, J.
Faberová, V.
Schmidtová, Ľ.
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| Title |
1-(2,6-Diisopropylphenyl)-3-(1,3-dimethyl-2,6-dioxo-2,3,6,7- tetrahydro-1H-purin-8/7-ylalkyl)ureas as Potential Acyl-CoA: Cholesterol Acyltransferase Inhibitors
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| Journal name |
Chemical Papers
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| Publication date |
2002
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| Year available |
2002
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| Volume number |
56
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| Issue number |
5
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| ISSN |
0366-6352
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| Start page |
330
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| End page |
339
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| Place of publication |
Poland
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| Publisher |
Versita
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| Collection year |
2002
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| Language |
english
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| Subject |
250000 Chemical Sciences
320000 Medical and Health Sciences
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| Abstract/Summary |
As potential hypocholesterolemics were synthesized 3-(7-alkyl-1,3-dimethyl-2,6-dioxo-2,3,6,7- tetrahydro-1H-purin-8-ylmethyl)- (I) and 3-[2-(1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin- 7-yl)ethyl]-1-(2,6-diisopropylphenyl)ureas (II ) from appropriate 8-(aminomethyl) or 7-(aminoethyl) derivatives and 2,6-diisopropylphenyl isocyanate. Similarly were prepared 3-alkyl/aryl/cycloalkyl-3- (7-alkyl-1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-ylmethyl)-1-(2,6-diisopropylphenyl)- ureas (III ) from appropriate 8-(alkyl-/aryl-/cycloalkylaminomethyl)purine-2,6-diones (X). The intermediates X were prepared starting from a suitable purine-8-carbaldehyde and primary amines via corresponding azomethines and their hydrogenation. The disubstituted and trisubstituted ureas I—III were evaluated for their ability to inhibit in vitro the activity of acyl-CoA:cholesterol acyltransferase, the key enzyme of cholesterol esterification.
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