Dual acting antioxidant A1 adenosine receptor agonists
Copyright policy )Dual acting antioxidant A1 adenosine receptor agonists
Herein we report the synthesis and biological evaluation of some potent and selective A(1) adenosine receptor agonists, which incorporate a functionalised linker attached to an antioxidant moiety. N(6)-(2,2,5,5-Tetramethylpyrrolidin-1-yloxyl-3-ylmethyl)adenosine (VCP28, 2e) proved to be an agonist with high affinity (K(i)=50nM) and good selectivity (A(3)/A(1) > or = 400) for the A(1) adenosine receptor. N(6)-[4-[2-[1,1,3,3-Tetramethylisoindolin-2-yloxyl-5-amido]ethyl]phenyl]adenosine (VCP102, 5a) has higher binding affinity (K(i)=7 nM), but lower selectivity (A(3)/A(1)= approximately 3). All compounds bind weakly (K(i)>1 microM) to A(2A) and A(2B) receptors. The combination of A(1) agonist activity and antioxidant activity has the potential to produce cardioprotective effects.
- University of Virginia United States
- Monash University Australia
- Monash University, Parkville campus Australia
- Queensland University of Technology Australia
Adenosine, Binding Sites, Cardiotonic Agents, Pyrrolidines, Myocardial Ischemia, Myocardial Reperfusion Injury, Isoindoles, Antioxidants, A1 Adenosine Receptor (A1AR) Agonist, Adenosine A1 Receptor Agonists, Cell Line, Rats, Structure-Activity Relationship, Xanthines, Animals, Indicators and Reagents, Myocytes, Cardiac, Antioxidant
Adenosine, Binding Sites, Cardiotonic Agents, Pyrrolidines, Myocardial Ischemia, Myocardial Reperfusion Injury, Isoindoles, Antioxidants, A1 Adenosine Receptor (A1AR) Agonist, Adenosine A1 Receptor Agonists, Cell Line, Rats, Structure-Activity Relationship, Xanthines, Animals, Indicators and Reagents, Myocytes, Cardiac, Antioxidant
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