Abstract
During the search for second-generation adenosine A(1) receptor antagonist alternatives to the clinical candidate 8-(3-oxa-tricyclo[3.2.1.0(2,4)]oct-6-yl)-1,3-dipropyl-3,7-dihydro-purine-2,6-dione (BG9719), we developed a series of novel xanthines substituted with norbornyl-lactones that possessed high binding affinities for adenosine A(1) receptors and in vivo activity.
MeSH terms
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Adenosine A1 Receptor Antagonists*
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Adenosine A2 Receptor Antagonists
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Adenosine A3 Receptor Antagonists
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Animals
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Binding, Competitive / drug effects
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Bridged Bicyclo Compounds / chemistry*
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Cell Line
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Humans
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Lactones / chemistry*
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Ligands
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Molecular Structure
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Norbornanes / chemical synthesis
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Norbornanes / chemistry
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Norbornanes / pharmacology*
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Rats
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Stereoisomerism
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Structure-Activity Relationship
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Xanthines / chemical synthesis
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Xanthines / chemistry
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Xanthines / pharmacology*
Substances
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Adenosine A1 Receptor Antagonists
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Adenosine A2 Receptor Antagonists
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Adenosine A3 Receptor Antagonists
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Bridged Bicyclo Compounds
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Lactones
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Ligands
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Norbornanes
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Xanthines
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norbornyllactone