Browsing by Author "10057072 - Bergh, Jacobus Johannes"

Now showing items 1-20 of 28

    • 2-Aminopyrimidines as dual adenosine A1/A2A antagonists 

      Robinson, Sarel J.; Petzer, Jacobus P.; Terre'Blanche, Gisella; Petzer, Anél; Van der Walt, Mietha M.; Bergh, Jacobus J.; Lourens, Anna C.U. (Elsevier, 2015)
      In this study thirteen 2-aminopyrimidine derivatives were synthesised and screened as potential antagonists of adenosine A1 and A2A receptors in order to further investigate the structure activity relationships of this ...

    • 8-Aryl- and alkyloxycaffeine analogues as inhibitors of monoamine oxidase 

      Strydom, Belinda; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2011)
      Recently it was reported that a series of 8-benzyloxycaffeine analogues are potent reversible inhibitors of human monoamine oxidase (MAO) A and B. In an attempt to discover additional C8 oxy substituents of caffeine that ...

    • 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. (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 ...

    • Die adenosien A1- en A2A-reseptoraffiniteit van ’n reeks 3,4-dihidropirimidoon-analoë 

      Katsidzira, Runako M.; Van der Walt, Mietha M.; Bergh, Jacobus J.; Terre'Blanche, Gisella (AOSIS, 2017)
      Parkinson se siekte is ’n komplekse neurodegeneratiewe siektetoestand. Huidige behandeling van dié siekte is slegs op simptomatiese verligting gemik, sonder dat die siekteverloop vertraag of gestop word. Sedert die ...

    • Die identifisering van fenielbottersuur aromatiese metaboliete in die urien van die blou-aap 

      Van der Linde, Wilhelmina J.; Mienie, Lodewyk J.; Bergh, Jacobus J.; Van der Walt, Mietha M.; Terre'Blanche, Gisella (Suid-Afrikaanse Akademie vir Wetenskap en Kuns, 2018)
      Phenylbutyrate (PBA) is used as treatment of urea cycle disorders and as an alternative treatment option for adrenoleykodystrophy, has neuroprotective effects and provides protection against oxidative stress. Known ...

    • 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; 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 (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 ...

    • The inhibition of monoamine oxidase by 8-(2-phenoxyethoxy) caffeine analogues 

      Strydom, B.; Bergh, J.J.; Petzer, J.P. (Thieme, 2012)
      Previous studies have documented that substituted 8-oxycaffeines act as inhibitors of human monoamine oxidase (MAO) B. A particularly potent inhibitor among the reported compounds was 8-(2-phenoxyethoxy)caffeine with an ...

    • Inhibition of monoamine oxidase by 8-[(phenylethyl)sulfanyl]caffeine analogues 

      Mostert, Samantha; Mentz, Wayne; Petzer, Anél; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2012)
      In a previous study we have investigated the monoamine oxidase (MAO) inhibitory properties of a series of 8-sulfanylcaffeine analogues. Among the compounds studied, 8-[(phenylethyl)sulfanyl]caffeine (IC50 = 0.223 lM) was ...

    • Inhibition of monoamine oxidase by 8-benzyloxycaffeine analogues 

      Strydom, Belinda; Malan, Sarel F.; Bergh, Jacobus J.; Petzer, Jacobus P.; Castagnoli, Neal (Elsevier, 2010)
      Based on recent reports that several (E)-8-styrylcaffeinyl analogues are potent reversible inhibitors of monoamine oxidase B (MAO-B), a series of 8-benzyloxycaffeinyl analogues were synthesized and evaluated as inhibitors ...

    • Inhibition of monoamine oxidase by 8-phenoxymethylcaffeine derivatives 

      Okaecwe, Thokozile; Swanepoel, Abraham J.; Petzer, Anél; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2012)
      A recent study has reported that a series of 8-benzyloxycaffeines are potent and reversible inhibitors of both human monoamine oxidase (MAO) isoforms, MAO-A and -B. In an attempt to discover additional caffeine derivatives ...

    • Inhibition of monoamine oxidase by C5-substituted phthalimide analogues 

      Manley-King, Clarina I.; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2011)
      Literature reports that isatin as well as C5- and C6-substituted isatin analogues are reversible inhibitors of human monoamine oxidase (MAO) A and B. In general, C5- and C6-substitution of isatin leads to enhanced binding ...

    • 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. (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 ...

    • Inhibition of monoamine oxidase by phthalide analogues 

      Strydom, Belinda; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2013)
      Based on recent reports that the small molecules, isatin and phthalimide, are suitable scaffolds for the design of high potency monoamine oxidase (MAO) inhibitors, the present study examines the MAO inhibitory properties ...

    • Inhibition of monoamine oxidase by selected C5- and C6-substituted isatin analogues 

      Manley-King, Clarina I.; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2011)
      Previous studies have shown that (E)-5-styrylisatin and (E)-6-styrylisatin are reversible inhibitors of human monoamine oxidase (MAO) A and B. Both homologues are reported to exhibit selective binding to the MAO-B isoform ...

    • Inhibition of monoamine oxidase by selected phenylalkylcaffeine analogues 

      Petzer, Anél; Grobler, Paul; Bergh, Jacobus J.; Petzer, Jacobus P. (Wiley, 2014)
      Objectives Caffeine represents a useful scaffold for the design of monoamine oxidase (MAO) type B inhibitors. Specifically, substitution on the C8 position yields structures which are high-potency MAO-B inhibitors. To ...

    • Inhibition of  monoamine oxidase by 8-benzyloxycaffeine analogues 

      Strydom, Belinda; Malan, Sarel F.; Bergh, Jacobus J.; Petzer, Jacobus P.; Castagnoli, Neal (Elsevier, 2010)
      Based on recent reports that several (E)-8-styrylcaffeinyl analogues are potent reversible inhibitors of monoamine oxidase B (MAO-B), a series of 8-benzyloxycaffeinyl analogues were synthesized and evaluated as inhibitors ...

    • Interactions of 1-methyl-3-phenylpyrrolidine and 3-methyl-1-phenyl-3-azabicyclo[3.1.0]hexane with monoamine oxidase B 

      Pretorius, Anél; Ogunrombi, Modupe O.; Fourie, Hendrik; Terre'blanche, Gisella; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2010)
      The parkinsonian inducing agent 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and its corresponding five-membered ring analogue 1-methyl-3-phenyl-3-pyrroline are cyclic tertiary allylamines and good substrates of ...

    • Investigating the potential neuroprotective effects of statins on DNA damage in mouse striatium 

      Coetsee, T.N.; Pretorius, P.J.; Terre'Blanche, G.; Bergh, J.J. (Elsevier, 2008)
      We investigated the protective effect of pravastatin, simvastatin and atorvastatin on striatal DNA damage as a potential method to conserve and protect the nigrostriatal neurons. C57Bl/J6 mice were treated with combinations ...

    • Monoamine oxidase inhibition by C4-substituted phthalonitriles 

      Manley-King, Clarina I.; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2012)
      It was recently reported that a series of C5-substituted phthalimides are remarkably potent reversible inhibitors of recombinant human monoamine oxidase (MAO) B. Modeling studies suggested that the phthalimide ring forms ...