Microwave assisted synthesis of spirocyclic pyrrolidines – σ1 receptor ligands with modified benzene-N-distance
Copyright policy )Microwave assisted synthesis of spirocyclic pyrrolidines – σ1 receptor ligands with modified benzene-N-distance
Two series of σ(1) ligands with a spiro[[2]benzopyran-1,3'-pyrrolidine] (3) and a spiro[[2]benzofuran-1,3'-pyrrolidine] (4) framework were synthesized and pharmacologically evaluated. Several reaction steps were considerably improved by microwave irradiation. The σ(1) affinity of the spirocyclic ligands correlates nicely with the benzene-N-distance, i.e. 2 40-fold), the NMDA receptor and 5-HT(6) and 5-HT(7) receptors. Moreover, 4a did not inhibit the hERG channel in the heart.
- University of Münster Germany
Pyrrolidines, Nitrogen, Guinea Pigs, Benzene, Chemistry Techniques, Synthetic, Ligands, Ether-A-Go-Go Potassium Channels, Substrate Specificity, Animals, Humans, Receptors, sigma, Spiro Compounds, Microwaves
Pyrrolidines, Nitrogen, Guinea Pigs, Benzene, Chemistry Techniques, Synthetic, Ligands, Ether-A-Go-Go Potassium Channels, Substrate Specificity, Animals, Humans, Receptors, sigma, Spiro Compounds, Microwaves
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