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Abstract
The anti Parkinson drug, rasagiline [R-(+)-N-propargyl-1-aminoindan], an inhibitor
of type B monoamine oxidase, has been shown to suppress apoptosis induced by neurotoxins
and oxidative stress. A series of novel propargylaminoindans with a carbamate moiety
to inhibit cholinesterase were developed from phamacophore of rasagiline to protect
or rescue deteriorated neurons in Alzheimer's and Lewy Body disease and provide a
beneficial effect on the cognitive deficits. Rasagiline analogues were found to protect
dopaminergic SH-SY5Y cells against apoptosis induced by peroxynitrite donor. SIN-1.
TV3326, [(N-propargyl)-(3R)-aminoindan-5-yl]-ethyl methyl carbamate, was as effective
as rasagiline in preventing apoptosis, followed by its S-enantiomer, TV3279. The anti-apoptotic-neuroprotective
activity was shown to reside in the propargylamine and not the carbamate moiety. This
resulted in stabilization of the mitochondrial membrane potential, the collapse of
which initiates the apoptotic cascade.