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Browsing Faculty of Health Sciences@PUK by Subject "reversible inhibition"

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Browsing Faculty of Health Sciences@PUK by Subject "reversible inhibition"

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  • Bergh, Jacobus Johannes; Petzer, Jacobus Petrus; Strydom, Belinda (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 ...
  • Meiring, Letitia; Petzer, Jacobus Petrus; 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 ...
  • Bergh, Jacobus Johannes; Petzer, Jacobus Petrus; Strydom, Belinda (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 ...
  • Bergh, Jacobus Johannes; Mentz, Wayne; Mostert, Samantha; Petzer, Jacobus Petrus; Petzer, Anél (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 ...
  • Bergh, Jacobus Johannes; Okaecwe, Thokozile Audrey Dorcas; Petzer, Jacobus Petrus; Swanepoel, Abraham Johannes; Petzer, Anél (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 ...
  • Bergh, Jacobus Johannes; Petzer, Jacobus Petrus; Manley-King, Clarina Ilara (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 ...
  • 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 ...
  • Bergh, Jacobus Johannes; Petzer, Jacobus Petrus; Manley-King, Clarina Ilara (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 ...
  • Legoabe, Lesetja Jan; Petzer, Jacobus Petrus; Kruger, Johann; Petzer, Anél; Bergh, Jacobus J. (Elsevier, 2012)
    Chromone has been reported to be a useful scaffold for the design of monoamine oxidase (MAO) inhibitors. In an attempt to discover highly potent MAO inhibitors and to contribute to the known structureeactivity relationships ...
  • Bergh, Jacobus Johannes; Petzer, Jacobus Petrus; Manley-King, Clarina Ilara (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 ...
  • Legoabe, Lesetja Jan; Petzer, Jacobus Petrus; Petzer, Anél (Elsevier, 2012)
    A previous study has shown that a series of C6-benzyloxy substituted chromones exhibit high binding affinities for human monoamine oxidase (MAO) B. In an attempt to discover additional chromones with potent and selective ...
  • Robinson, Sarel J.; Petzer, Jacobus P.; Petzer, Anél; Bergh, Jacobus J.; Lourens, Anna C. U. (ELSEVIER, 2013)
    The validity of the chalcone scaffold for the design of inhibitors of monoamine oxidase has previously been illustrated. In a systematic attempt to investigate the effect of heterocyclic substitution on the monoamine ...
  • Bergh, Jacobus Johannes; Booysen, Hermanus Perold; Moraal, Christina Maria; Petzer, Jacobus Petrus; Petzer, Anél; Terre'Blanche, Gisella (Elsevier, 2011)
    In a recent study it was shown that 8-benzyloxycaffeine analogues act as potent reversible inhibitors of human monoamine oxidase (MAO) A and B. Although the benzyloxy side chain appears to be particularly favorable for ...

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