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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
2000-11-14
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pubmed:abstractText |
The synthesis of oximeethers of 2,3-dihydro-1,8-naphthyridine and 2, 3-dihydrothiopyrano[2,3-b]pyridine is described. These compounds exhibit a selective beta-blocking activity, with a selectivity towards beta(2)-receptors. Groups in the N(1) position giving rise to a considerable steric hindrance led to a higher beta(2)-blocking selectivity, whereas groups creating a moderate hindrance caused a weak but significant decrease in beta(2)-antagonist potency. Substitution of the N(1)-R group with a sulfur atom led to compounds possessing beta(1)-, beta(2)- and beta(3)-blocking properties. Compounds 9c(1) and 10a(1) showed a beta(3)-antagonist activity slightly lower than that of propranolol.
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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/Adrenergic beta-Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Antihypertensive Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Isoproterenol,
http://linkedlifedata.com/resource/pubmed/chemical/Naphthyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrans,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-2,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, beta-3
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pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0223-5234
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
35
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
815-26
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:11006483-Adipose Tissue,
pubmed-meshheading:11006483-Adrenergic beta-Antagonists,
pubmed-meshheading:11006483-Animals,
pubmed-meshheading:11006483-Antihypertensive Agents,
pubmed-meshheading:11006483-Drug Evaluation, Preclinical,
pubmed-meshheading:11006483-Guinea Pigs,
pubmed-meshheading:11006483-Inhibitory Concentration 50,
pubmed-meshheading:11006483-Isoproterenol,
pubmed-meshheading:11006483-Male,
pubmed-meshheading:11006483-Naphthyridines,
pubmed-meshheading:11006483-Pyrans,
pubmed-meshheading:11006483-Pyridines,
pubmed-meshheading:11006483-Rats,
pubmed-meshheading:11006483-Rats, Wistar,
pubmed-meshheading:11006483-Receptors, Adrenergic, beta-1,
pubmed-meshheading:11006483-Receptors, Adrenergic, beta-2,
pubmed-meshheading:11006483-Receptors, Adrenergic, beta-3,
pubmed-meshheading:11006483-Structure-Activity Relationship
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pubmed:year |
2000
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pubmed:articleTitle |
Synthesis and beta-blocking activity of (R,S)-(E)-oximeethers of 2, 3-dihydro-1,8-naphthyridine and 2,3-dihydrothiopyrano[2, 3-b]pyridine:potential antihypertensive agents - part IX.
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pubmed:affiliation |
Dipartimento di Scienze Farmaceutiche, Università di Pisa, via Bonanno 6, 56126, Pisa, Italy. ferrarini@farm.unipi.it
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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