Now showing items 1-8 of 8

    • The adenosine receptor affinities and monoamine oxidase B inhibitory properties of sulfanylphthalimide analogues 

      Van der Walt, Mietha M.; Terre'Blanche, Gisella; Petzer, Anél; Petzer, Jacobus P. (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- ...
    • Deuterium isotope effects for the oxidation of 1-methyl-3phenyl-3pyrrolinyl analogues by monoamine oxidase B 

      Pretorius, Anél; Ogunrombi, Modupe O.; Terre'Blanche, Gisella; Bergh, Jacobus J.; Petzer, Jacobus P.; Pretorius, Anél; Ogunrombi, Modupe O.; Terre'Blanche, Gisella; Bergh, Jacobus J.; Petzer, Jacobus P. (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 

      Malan, Sarel F.; Bergh, Jacobus J.; Petzer, Jacobus P.; Castagnoli, Neal; Malan, Sarel F.; Bergh, Jacobus J.; Petzer, Jacobus P.; Castagnoli, Neal; Pretorius, Judey (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 ...
    • Inhibition of monoamine oxidase B by N-methyl-2-phenylmaleimides 

      Manley-King, Clarina I.; Terre'blanche, Gisella; Bergh, Jacobus J.; Petzer, Jacobus P.; Castagnoli, Neal; Manley-King, Clarina I.; Terre'blanche, Gisella; Bergh, Jacobus J.; Petzer, Jacobus P.; Castagnoli, Neal (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 

      Van der Walt, Elizna M.; Bergh, Jacobus J.; Petzer, Jacobus P.; Malan, Sarel F.; Milczek, E.M.; Van der Walt, Elizna M.; Bergh, Jacobus J.; Petzer, Jacobus P.; Malan, Sarel F.; Milczek, E.M. (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 

      Legoabe, Lesetja; Kruger, Johann; Petzer, Anél; Bergh, Jacobus J.; Petzer, Jacobus P.; Legoabe, Lesetja; Kruger, Johann; Petzer, Anél; Bergh, Jacobus J.; Petzer, Jacobus P. (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 

      Ogunrombi, Modupe O.; Malan, Sarel F.; Terre'Blanche, Gisella; Bergh, Jacobus J.; Petzer, Jacobus P.; Ogunrombi, Modupe O.; Malan, Sarel F.; Terre'Blanche, Gisella; Bergh, Jacobus J.; Petzer, Jacobus P. (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 ...
    • Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxice synthase inhibitors 

      Prins, Louis H.A.; Petzer, Jacobus P.; Malan, Sarel F.; Prins, Louis H.A.; Petzer, Jacobus P.; Malan, Sarel F. (Elsevier, 2009)
      Monoamine oxidase B (MAO-B) and nitric oxide synthase (NOS) have both been implicated in the pathology of neurodegenerative diseases. In an attempt to design dual-target-directed drugs that inhibit both these enzymes, a ...