Neuroprotective Tri- and
Tetracyclic BChE Inhibitors
Releasing Reversible Inhibitors upon Carbamate Transfer
Posted on 2012-11-08 - 00:00
Tri- and tetracyclic nitrogen-bridgehead compounds were
designed
and synthesized to yield micromolar cholinesterase (ChE) inhibitors.
Structure–activity relationships identified potent compounds
with butyrylcholinesterase selectivity. These compounds were selected
as starting points for the design and synthesis of carbamate-based
(pseudo)irreversible inhibitors. Compounds with superior inhibitory
activity and selectivity were obtained and kinetically characterized
also with regard to the velocity of enzyme carbamoylation. Structural
elements were identified and introduced that additionally showed neuroprotective
properties on a hippocampal neuronal cell line (HT-22) after glutamate-induced
intracellular reactive oxygen species generation. We have identified
potent and selective pseudoirreversible butyrylcholinesterase inhibitors
that release reversible inhibitors with neuroprotective properties
after carbamate transfer to the active site of cholinesterases.
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Darras, Fouad
H.; Kling, Beata; Heilmann, Jörg; Decker, Michael (2016). Neuroprotective Tri- and
Tetracyclic BChE Inhibitors
Releasing Reversible Inhibitors upon Carbamate Transfer. ACS Publications. Collection. https://doi.org/10.1021/ml3001825
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AUTHORS (4)
FD
Fouad
H. Darras
BK
Beata Kling
JH
Jörg Heilmann
MD
Michael Decker