Browsing Faculty of Health Sciences by Subject "Competitive"

Now showing items 1-10 of 10

    • 3-Coumaranone derivatives as inhibitors of monoamine oxidase 

      Van Dyk, Adriaan S.; Petzer, Jacobus P.; Petzer, Anél; Legoabe, Lesetja J. (Dove Press, 2015)
      The present study examines the monoamine oxidase (MAO) inhibitory properties of a series of 20 3-coumaranone [benzofuran-3(2H)-one] derivatives. The 3-coumaranone derivatives are structurally related to series of α-tetralone ...

    • Evaluation of natural and synthetic 1,4-naphthoquinones as inhibitors of monoamine oxidase 

      Mostert, Samantha; Petzer, Anél; Petzer, Jacobus P. (Wiley, 2016)
      Previous reports have documented that 1,4-naphtho- quinones act as inhibitors of the monoamine oxidase (MAO) enzymes. In particular, fractionation of the extracts of cured tobacco leafs has led to the charac- terization ...

    • 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 ...

    • The inhibition of monoamine oxidase by esomeprazole 

      Petzer, A.; Pienaar, A.; Petzer, J.P. (Thieme, 2013)
      Virtual screening of a library of drugs has suggested that esomeprazole, the S-enantiomer of omeprazole, may possess binding affinities for the active sites of the monoamine oxidase (MAO) A and B enzymes. Based on this ...

    • 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 ...

    • The interactions of caffeine with monoamine oxidase 

      Petzer, Anél; Pienaar, Anke; Petzer, Jacobus P. (Elsevier, 2013)
      Aims: Caffeine has been used as a scaffold for the design of inhibitors of monoamine oxidase (MAO) A and B. Substitution at the C8 position with a variety of moieties yields structures with high MAO inhibition ...

    • Monoamine oxidase inhibitory activities of heterocyclic chalcones 

      Minders, Corné; Petzer, Jacobus P.; Petzer, Anél; Lourens, Anna C.U. (Elsevier, 2015)
      Studies have shown that natural and synthetic chalcones (1,3-diphenyl-2-propen-1-ones) possess monoamine oxidase (MAO) inhibition activities. Of particular importance to the present study is a report that a series of ...

    • Selected furanochalcones as inhibitors of monoamine oxidase 

      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 ...

    • The synthesis and evaluation of C7-substituted α-tetralone derivatives as inhibitors of monoamine oxidase 

      Legoabe, Lesetja J.; Petzer, Anél; Petzer, Jacobus P. (Wiley, 2015)
      Based on a previous report that α-tetralone (3,4-dihydro-2H-naphthalen-1-one) is a promising scaffold for the design of highly potent inhibitors of the enzyme, monoamine oxidase, the present study investigates the monoamine ...

    • Synthesis and evaluation of chromone derivatives as inhibitors of monoamine oxidase 

      Mpitimpiti, Annah N.; Petzer, Jacobus P.; Petzer, Anél; Jordaan, Johannes H.L.; Lourens, Anna C.U. (Springer, 2019)
      Based on reports that chromone compounds are good potency inhibitors of monoamine oxidase (MAO), the present study evaluates the effect of substitution with flexible side chains on the 3 position on MAO inhibition potency. ...