Browsing by Subject "Structure-activity relationship"

Now showing items 1-10 of 14

    • 2-Acetylphenol analogs as potent reversible monoamine oxidase inhibitors 

      Legoabe, Lesetja J.; Petzer, Anél; Petzer, Jacobus P. (Dove Press, 2015)
      Based on a previous report that substituted 2-acetylphenols may be promising leads for the design of novel monoamine oxidase (MAO) inhibitors, a series of C5-substituted 2-acetylphenol analogs (15) and related compounds ...

    • 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 ...

    • 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. (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 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 C6-substituted chromone derivatives 

      Legoabe, Lesetja J.; Petzer, Anél; Petzer, Jacobus P. (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 ...

    • 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 ...

    • Monoamine oxidase inhibition by novel quinolinones 

      Meiring, Letitia (2014)
      Parkinson’s disease (PD) is an age-related neurodegenerative disorder. The degeneration of the neurons of the substantia nigra in the midbrain leads to the loss of dopamine from the striatum, which is responsible for the ...

    • Selected C7-substituted chromone derivatives as monoamine oxidase inhibitors 

      Legoabe, Lesetja J.; Petzer, Anél; Petzer, Jacobus P. (Elsevier, 2012)
      A series of C7-substituted chromone (1-benzopyran-4-one) derivatives were synthesized and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. The chromones are structurally related to a series of ...