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Development of Bicyclo[3.1.0]hexane-based A3 Receptor Ligands – Closing the Gaps in the Structure-affinity Relationships

A peer-reviewed version of this preprint was published in:
Molecules 2022, 27(7), 2283. https://doi.org/10.3390/molecules27072283

Submitted:

09 March 2022

Posted:

10 March 2022

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Abstract
In this paper, a series of bicyclo[3.1.0]hexane-based nucleosides were synthesized and evaluated for their P1 receptor affinities in radioligand binding studies. The most potent derivative 30 displayed moderate A3AR affinity (Ki of 0.38 μM) and high A3R selectivity. A subset of compounds varied at 5’-position was further evaluated in functional P2Y1R assays displaying no off-target activity.
Keywords: 
Adenosine receptors
;  
methanocarba
;  
bicyclo[3.1.0]hexane
;  
A3 receptors
Subject: 
Chemistry and Materials Science  -   Medicinal Chemistry
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