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 B...

Rasagiline (N-propargyl-1 (R)-aminoindan) is a novel propargylamine, irreversible, selective monoamine oxidase inhibitor for treatment of Parkinson's disease (PD), a progressive condition associated with degeneration of dopaminergic neurons in the substantia nigra. Rasagiline inhibits striatal dopamine metabolism, thereby providing relief from motor symptoms of PD. It may be dosed once daily an...

Methamphetamine (METH) abuse is a serious health and social problem worldwide. At present, however, there are no effective medications for the treatment of METH abuse. Of the intracellular METH target proteins, monoamine oxidase (MAO) is involved in the regulation of monoaminergic tone in the brain, resulting in the modulation of METH-induced behavioral abnormalities in mammals. The METH-induce...

Based on ursolic acid, 3 compounds with isothiocyanate groups located at different distances from C-17 of the triterpenoid core have been synthesized through ursane-derived primary amines. To obtain terpene hybrids thioureas and N,S-containing heterocycles, series amines ammonia were reacted novel isothiocyanates. In reactions propargylamine, 4,5-dihydrothiazol-2-yl-amine selectively obtained i...

Density functional theory (DFT) was used to investigate the three-component coupling reactions of aldehydes, alkynes, and amines (A3 coupling) using N-heterocyclic carbene silver as catalyst. This study reveals that addition reaction between catalyst phenylacetylene (PAE) forms Ag_PAE. Subsequently, one hydrogen atom Ag_PAE migrates nitrogen Amine. Thereafter, amine aldehyde condensation genera...

(R)-N-(2-Heptyl)-N-methylpropargylamine (R-2HMP) is a monoamine oxidase inhibitor and putative antiapoptotic agent analogous to (R)-deprenyl. In the rat, the major amine metabolites of R-2HMP have been identified as (R)-N-2-heptylmethylamine (R-2HMA), (R)-N-2-heptylpropargylamine (R-2HPA), and (R)-2-heptylamine (R-2HA). After R-2HMP was administered s.c. to male Wistar rats, it was observed tha...