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- W1970043402 abstract "Abstract A set of racemic spirocyclic quinuclidinyl‐Δ 2 ‐isoxazoline derivatives was synthesized using a 1,3‐dipolar cycloaddition‐based approach. Target compounds were assayed for binding affinity toward rat neuronal homomeric (α7) and heteromeric (α4β2) nicotinic acetylcholine receptors. Δ 2 ‐Isoxazolines 3 a (3‐Br), 6 a (3‐OMe), 5 a (3‐Ph), 8 a (3‐O n Pr), and 4 a (3‐Me) were the ligands with the highest affinity for the α7 subtype ( K i values equal to 13.5, 14.2, 25.0, 71.6, and 96.2 n M , respectively), and showed excellent α7 versus α4β2 subtype selectivity. These compounds, tested in electrophysiological experiments against human α7 and α4β2 receptors stably expressed in cell lines, behaved as partial α7 agonists with varying levels of potency. The two enantiomers of (±)‐3‐methoxy‐1‐oxa‐2,7‐diaza‐7,10‐ethanospiro[4.5]dec‐2‐ene sesquifumarate 6 a were prepared using (+)‐dibenzoyl‐ L ‐ or (−)‐dibenzoyl‐ D ‐tartaric acid as resolving agents. Enantiomer ( R )‐(−)‐ 6 a was found to be the eutomer, with K i values of 4.6 and 48.7 n M against rat and human α7 receptors, respectively." @default.
- W1970043402 created "2016-06-24" @default.
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- W1970043402 date "2011-03-01" @default.
- W1970043402 modified "2023-10-16" @default.
- W1970043402 title "Design, Synthesis, and Pharmacological Characterization of Novel Spirocyclic Quinuclidinyl-Δ2-Isoxazoline Derivatives as Potent and Selective Agonists of α7 Nicotinic Acetylcholine Receptors" @default.
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- W1970043402 doi "https://doi.org/10.1002/cmdc.201000514" @default.
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