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

Jan Phillip Lemmerhirt; Andreas Isaak; Rongfang Liu; Max Kock; Constantin G. Daniliuc; Kenneth A. Jacobson; Laura H. Heitman; Anna Junker

doi:10.20944/preprints202203.0157.v1

A peer-reviewed article of this Preprint also exists.

Lemmerhirt, J.P.; Isaak, A.; Liu, R.; Kock, M.; Daniliuc, C.G.; Jacobson, K.A.; Heitman, L.H.; Junker, A. Development of Bicyclo[3.1.0]hexane-Based A₃ Receptor Ligands: Closing the Gaps in the Structure–Affinity Relationships. Molecules 2022, 27, 2283. Lemmerhirt, J.P.; Isaak, A.; Liu, R.; Kock, M.; Daniliuc, C.G.; Jacobson, K.A.; Heitman, L.H.; Junker, A. Development of Bicyclo[3.1.0]hexane-Based A3 Receptor Ligands: Closing the Gaps in the Structure–Affinity Relationships. Molecules 2022, 27, 2283.

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.

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

Abstract

Keywords

Subject

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