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- LH_-_Synthesis_and_SAR_evaluation_of_coumarin_derivatives_as_potent_cannabinoid_receptor
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Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists
modified coumarins as cannabinoid receptor ligands. In radioligand, and [35S]GTPgS binding assays the
CB receptor binding affinities and efficacies of the new ligands were determined. Furthermore, we used a
ligand-based docking approach to validate the empirical observed results. In conclusion, several crucial
structural requirements were identified. The most potent coumarins like 3-butyl-7-(1-butylcyclopentyl)-
5-hydroxy-2H-chromen-2-one (36b, Ki CB2 13.7 nM, EC50 18 nM), 7-(1-butylcyclohexyl)-5-hydroxy-3-
propyl-2H-chromen-2-one (39b, Ki CB2 6.5 nM, EC50 4.51 nM) showed a CB2 selective agonistic profile
with low nanomolar affinities.
- All authors
- Mohr, F.; Hurrle, T.; Burggraaff, L.; Langer, L.; Bemelmans, M.P.; Knab, M.; Nieger, M.; Westen, G.J.P. van; Heitman, L.H.; Bräse, S.
- Date
- 2021-04-07
- Volume
- 220