Dual acting antioxidant A1 adenosine receptor agonists
Gregg, Alison D., Bottle, Steven E., Devine, Shane M., Figler, Heidi, Linden, Joel, White, Paul, Pouton, Colin W., Urmaliya, Vijay, & Scammells, Peter J. (2007) Dual acting antioxidant A1 adenosine receptor agonists. Bioorganic & Medicinal Chemistry Letters, 17(9), pp. 5437-5441.
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Abstract
Herein we report the synthesis and biological evaluation of some potent and selective A1 adenosine receptor agonists, which incorporate a functionalised linker attached to an antioxidant moiety. N6-(2,2,5,5-Tetramethylpyrrolidin-1-yloxyl-3-ylmethyl)adenosine (VCP28, 2e) proved to be an agonist with high affinity (Ki = 50 nM) and good selectivity (A3/A1 400) for the A1 adenosine receptor. N6-[4-[2-[1,1,3,3-Tetramethylisoindolin-2-yloxyl-5-amido]ethyl]phenyl]adenosine (VCP102, 5a) has higher binding affinity (Ki = 7 nM), but lower selectivity (A3/A1 = 3). All compounds bind weakly (Ki > 1 μM) to A2A and A2B receptors. The combination of A1 agonist activity and antioxidant activity has the potential to produce cardioprotective effects.
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| ID Code: | 15127 |
|---|---|
| Item Type: | Journal Article |
| Keywords: | Adenosine, Antioxidant, A1 adenosine receptor (A1AR) agonist |
| DOI: | 10.1016/j.bmcl.2007.07.035 |
| ISSN: | 0960-894X |
| Subjects: | Australian and New Zealand Standard Research Classification > CHEMICAL SCIENCE (030000) > MEDICINAL AND BIOMOLECULAR CHEMISTRY (030400) > Medicinal and Biomolecular Chemistry not elsewhere classified (030499) |
| Divisions: | Past > QUT Faculties & Divisions > Faculty of Science and Technology |
| Copyright Owner: | Copyright 2007 Elsevier |
| Copyright Statement: | Reproduced in accordance with the copyright policy of the publisher. |
| Deposited On: | 13 Oct 2008 |
| Last Modified: | 29 Feb 2012 23:37 |
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