Abstract
The synthesis and SAR of 5-heterocycle-substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and selectivity for the A2B and A3 receptors. One compound (5f) shows good ADME properties in the rat and as such may be an important new compound in testing the current hypotheses proposing a therapeutic role for a dual A2B/A3 antagonist in allergic diseases.
MeSH terms
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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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Heterocyclic Compounds / chemical synthesis
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Heterocyclic Compounds / pharmacokinetics
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Heterocyclic Compounds / pharmacology
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Rats
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Rats, Wistar
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Receptor, Adenosine A2B / metabolism*
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Receptor, Adenosine A3 / metabolism*
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Structure-Activity Relationship
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Thiazoles* / chemical synthesis
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Thiazoles* / pharmacokinetics
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Thiazoles* / pharmacology
Substances
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Adenosine A2 Receptor Antagonists
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Adenosine A3 Receptor Antagonists
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Heterocyclic Compounds
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Receptor, Adenosine A2B
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Receptor, Adenosine A3
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Thiazoles