Forcing the phenyl moiety into the axial position by embedding the 2-phenyl-1,3-dioxane system in a tricyclic benzomorphan scaffold: design, synthesis and biological evaluation
Nina Schulte-Gauczinski, Judith Schmidt, Jens Köhler, Dirk Schepmann et autres
) = 6.4 nM, 9-fold selectivity) represents the most promising ligand. The highest ligand-lipophilicity efficiency (LLE) was obtained for the secondary cyclohexylmethylamine 3d (LLE = 6.7). However, the highest metabolic stability (phase I metabolism) was determined for the benzylamine 3b (89% intact …
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Organic & Biomolecular Chemistry