Browsing by Subject "Monoamine oxidase B"
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The adenosine receptor affinities and monoamine oxidase B inhibitory properties of sulfanylphthalimide analogues
(Elsevier, 2015)Based on a report that sulfanylphthalimides are highly potent monoamine oxidase (MAO) B selective inhibitors, the present study examines the adenosine receptor affinities and MAO-B inhibitory properties of a series of 4- ... -
Affinity of dihydropyrimidone analogues for adenosine A1 and A2A receptors
(2014)Parkinson’s disease (PD) is a neurodegenerative disorder that is characterised by a reduction of dopamine concentration in the striatum due to degeneration of dopaminergic neurons in the substantia nigra. Currently, first ... -
Deuterium isotope effects for the oxidation of 1-methyl-3phenyl-3pyrrolinyl analogues by monoamine oxidase B
(Elsevier, 2008)The parkinsonian inducing agent, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), is a cyclic tertiary allylamine exhibiting good monoamine oxidase B (MAO-B) substrate properties. MAO-B catalyzes the ring α-carbon ... -
Dual inhibition of monoamine oxidase B and antagonism of the adenosine A2A receptor by (E,E)-8-(4phenylbytadien-1-yl) caffeine analogues
(Elsevier, 2008)The adenosine A2A receptor has emerged as an attractive target for the treatment of Parkinson’s disease (PD). Evidence suggests that antagonists of the A2A receptor (A2A antagonists) may be neuroprotective and may help to ... -
Dual-target-directed drugs that block monoamine oxidase B and adenosine A2A receptors for Parkinson’s disease
(Springer, 2009)Inadequacies of the current pharmacotherapies to treat Parkinson’s disease (PD) have prompted efforts to identify novel drug targets. The adenosine A2A receptor is one such target. Antagonists of this receptor (A2A ... -
Inhibition of monoamine oxidase B by N-methyl-2-phenylmaleimides
(Elsevier, 2009)Based on a recent report that 1-methyl-3-phenylpyrrolyl analogues are moderately potent reversible inhibitors of the enzyme monoamine oxidase B (MAO-B), a series of structurally related N-methyl-2-phenylmaleimidyl analogues ... -
Inhibition of monoamine oxidase by E-styrylisatin analogues
(Elsevier, 2009)Previous studies have shown that (E)-8-(3-chlorostyryl)caffeine (CSC) is a specific reversible inhibitor of human monoamine oxidase B (MAO-B) and does not bind to human MAO-A. Since the small molecule isatin is a natural ... -
Monoamine oxidase inhibition by selected anilide derivatives
(Elsevier, 2011)A series of anilide derivatives were synthesized and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. The most potent inhibitors among the derivatives that were initially evaluated were ... -
Structure-activity relationships in the inhibition of monoamine oxidase B by 1-methyl-3-phenylpyrroles
(Elsevier, 2008)1-Methyl-3-phenyl-3-pyrrolines are structural analogues of the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and like MPTP are selective substrates of monoamine oxidase B (MAO-B). As part of an ongoing ... -
The synthesis and evaluation of 1-methyl-3-pyrrolines and 1-methylpyrroles as substrates and inhibitors of monoamine oxidase B
(North-West University, 2007)Very little is known about why and how the Parkinson's disease (PD) neurodegenerative process begins and progresses. In the course of developments for treatment of PD, the discovery of the inhibition of monoamine oxidase ...