Abstract
The synthesis and SAR of a series of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent A(2B) adenosine receptor antagonists is described. Several compounds showed good selectivity versus other adenosine receptors. The potent and selective analogue 9 was shown to have good oral bioavailability in the rat.
Copyright 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Adenosine A2 Receptor Antagonists*
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Administration, Oral
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Amides / chemical synthesis
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Amides / chemistry*
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Amides / pharmacokinetics
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Animals
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Anti-Asthmatic Agents / chemical synthesis
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Anti-Asthmatic Agents / chemistry*
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Anti-Asthmatic Agents / pharmacokinetics
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Drug Discovery
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Humans
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Microsomes, Liver / metabolism
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Pyridines / chemical synthesis
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Pyridines / chemistry*
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Pyridines / pharmacology
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology
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Rats
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Receptor, Adenosine A2B / metabolism
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Structure-Activity Relationship
Substances
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Adenosine A2 Receptor Antagonists
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Amides
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Anti-Asthmatic Agents
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Pyridines
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Pyrimidines
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Receptor, Adenosine A2B