Abstract
A series of new selective, high affinity A(1)-AdoR agonists is reported. Compound 23 that incorporated a carboxylic acid functionality in the 4-position of the pyrazole ring displayed K(iL) value of 1 nM for the A(1)-AdoR and >5000-fold selectivity over the A(3) and A(2A)-AdoRs. In addition, compound 19 that incorporated a carboxamide functionality in the 4-position of the pyrazole ring displayed subnanomolar affinity for the A(1)-AdoR (K(iL)=0.6 nM) and >600-fold selectivity over the A(3) and A(2A)-AdoRs.
MeSH terms
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Adenosine / analogs & derivatives*
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Adenosine / chemistry*
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Adenosine / pharmacology
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Adenosine A1 Receptor Agonists*
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Anti-Arrhythmia Agents / chemistry*
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Anti-Arrhythmia Agents / pharmacology
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Humans
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Hypolipidemic Agents / chemistry*
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Hypolipidemic Agents / pharmacology
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Molecular Structure
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Pyrazoles / chemistry*
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Pyrazoles / pharmacology
Substances
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Adenosine A1 Receptor Agonists
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Anti-Arrhythmia Agents
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Hypolipidemic Agents
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N-cyclopentyl-2-(4-carbamoylpyrazol-1-yl)adenosine
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N-norbornyl-2-(4-carboxypyrazol-1-yl)adenosine
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Pyrazoles
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Adenosine