Iminosugars as a new class of cholinesterase inhibitors.

Camille Decroocq , Fabien Stauffert , Olivier Pamlard (1) , Farah Oulaïdi , Estelle Gallienne , Olivier R Martin , Catherine Guillou (1) , Philippe Compain

1 ICSN - Institut de Chimie des Substances Naturelles

To further extend the scope of iminosugar biological activity, a systematic structure-activity relationship investigation has been performed by synthesizing and evaluating as cholinesterase inhibitors a library of twenty-three iminoalditols with different substitutions and stereochemistry patterns. These compounds have been evaluated in vitro for the inhibition of cholinesterases (different sources of acetylcholinesterase and butyrylcholinesterase). Some compounds have IC50 values in the micromolar range and display significant inhibition selectivity for butyrylcholinesterase over acetylcholinesterase. These are the first examples of iminosugar-based inhibitors of cholinesterases.

Domaines: Chimie

Camille Decroocq, Fabien Stauffert, Olivier Pamlard, Farah Oulaïdi, Estelle Gallienne, et al.. Iminosugars as a new class of cholinesterase inhibitors.. Bioorganic and Medicinal Chemistry Letters, 2015, 25 (4), pp.830-833. ⟨hal-01138284⟩