rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
1989-1-12
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pubmed:abstractText |
Several analogues of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzodioxa n (WB 4101, 1) were prepared and evaluated for their blocking activity on alpha 1- and alpha 2-adrenoreceptors in the isolated rat vas deferens. The results were compared with those obtained for 1 and benoxathian (2). It was shown that the two oxygens at positions 1 and 4 may have a different role in receptor binding. It seems that the oxygen at position 4 as such does not contribute to the binding while it is important in stabilizing an optimal conformation for drug-receptor interaction mechanism. On the other hand, the oxygen at position 1 might interact with a receptor polar pocket of reduced size by way of a donor-acceptor dipolar interaction. Furthermore, it was shown that replacement of the dehydrodioxane ring of 1 by a phenyl or a pyrrole nucleus causes a significant decrease in activity.
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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/(2-(2',6'-dimethoxy)phenoxyethylamin...,
http://linkedlifedata.com/resource/pubmed/chemical/Adrenergic alpha-Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Clonidine,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxanes,
http://linkedlifedata.com/resource/pubmed/chemical/Dioxins,
http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine,
http://linkedlifedata.com/resource/pubmed/chemical/Oxathiins,
http://linkedlifedata.com/resource/pubmed/chemical/Oxygen,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfur,
http://linkedlifedata.com/resource/pubmed/chemical/benoxathian
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
31
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2300-4
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:2903932-Adrenergic alpha-Antagonists,
pubmed-meshheading:2903932-Animals,
pubmed-meshheading:2903932-Binding Sites,
pubmed-meshheading:2903932-Chemical Phenomena,
pubmed-meshheading:2903932-Chemistry,
pubmed-meshheading:2903932-Clonidine,
pubmed-meshheading:2903932-Dioxanes,
pubmed-meshheading:2903932-Dioxins,
pubmed-meshheading:2903932-Male,
pubmed-meshheading:2903932-Muscle Contraction,
pubmed-meshheading:2903932-Norepinephrine,
pubmed-meshheading:2903932-Oxathiins,
pubmed-meshheading:2903932-Oxygen,
pubmed-meshheading:2903932-Rats,
pubmed-meshheading:2903932-Structure-Activity Relationship,
pubmed-meshheading:2903932-Sulfur,
pubmed-meshheading:2903932-Vas Deferens
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pubmed:year |
1988
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pubmed:articleTitle |
Structure-activity relationships in 1,4-benzodioxan-related compounds. Investigation on the role of the dehydrodioxane ring on alpha 1-adrenoreceptor blocking activity.
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pubmed:affiliation |
Department of Chemical Sciences, University of Camerino, Italy.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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