Now showing items 1-10 of 20

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

      Strydom, Belinda; Bergh, Jacobus J.; Petzer, Jacobus P.; 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 ...
    • Azure B and a synthetic structural analogue of methylene blue, ethylthioninium chloride, present with antidepressant-like properties 

      Delport, Anzelle; Harvey, Brian H.; Petzer, Anél; Petzer, Jacobus P. (Elsevier, 2014)
      Aims: The phenothiazinium compound, methylene blue (MB), possesses diverse pharmacological actions and is attracting attention for the treatment of bipolar disorder and Alzheimer's disease. MB acts on both monoamine oxidase ...
    • C6- and C7-substituted 3,4-dihydro-2(1H)-quinolinones as inhibitors of monoamine oxidase 

      Meiring, Letitia; Petzer, Jacobus Petrus; Petzer, Anél (Thieme, 2017)
      Purpose Monoamine oxidase (MAO) inhibitors are considered to be useful therapeutic agents and isoform specific inhibitors are employed for the treatment of depression and Parkinson’s disease. MAO inhibitors are also under ...
    • 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 by 3,4-dihydro-2(1H)-quinolinone derivatives 

      Meiring, Letitia; Petzer, Jacobus P.; Petzer, Anél (Elsevier, 2013)
      In the present study, a series of 3,4-dihydro-2(1H)-quinolinone derivatives were synthesized and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. The 3,4-dihydro-2(1H)- quinolinone derivatives ...
    • The inhibition of monoamine oxidase by 8-(2-phenoxyethoxy) caffeine analogues 

      Strydom, B.; Bergh, J.J.; Petzer, J.P.; 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.; 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; 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.; 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.; 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 ...