Now showing items 1-10 of 15

    • 8-(3-phenylpropyl)-1,3,7-triethylxanthine is a synthetic caffeine substitute with stronger metabolic modulator activity 

      Carrageta, David F.; Van der Walt, Mietha M.; Terre'Blanche, Gisella; Dias, Tânia R.; Jarak, Ivana (Elsevier, 2018)
      Caffeine is one of the most worldwide consumed methylxanthines. It is well-known for its thermogenic and cell metabolism modulating effects. Based on methylxanthines' chemical structure, 8-(3-phenylpropyl)-1,3,7-triethylxanthine ...
    • 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 ...
    • Discovery of 1,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine derivatives as novel adenosine A1 and A2A receptor antagonists 

      Harmse, Rozanne; Van der Walt, Mietha M.; Petzer, Jacobus P.; Terre'Blanche, Gisella (Elsevier, 2016)
      Based on a previous report that a series of 8-(phenoxymethyl)-xanthines may be promising leads for the design of A1 adenosine receptor antagonists, selected novel and known 1,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine ...
    • 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 ...
    • 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 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; 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 ...