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.

DOI: 10.3390/molecules27072283

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

Subject

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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

Abstract

Keywords

Subject

Comments (0)