Now showing items 1-10 of 21

    • 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 ...
    • 2-Benzylidene-1-indanone derivatives as inhibitors of monoamine oxidase 

      Nel, Magdalena S.; Petzer, Anél; Petzer, Jacobus P.; Legoabe, Lesetja J. (Elsevier, 2016)
      In the present study, a series of twenty-two 2-benzylidene-1-indanone derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. The 2-benzylidene-1-indanone derivatives ...
    • 2-Heteroarylidene-1-indanone derivatives as inhibitors of monoamine oxidase 

      Nel, Magdalena S.; Petzer, Anél; Petzer, Jacobus P.; Legoabe, Lesetja J. (Elsevier, 2016)
      In the present study a series of fifteen 2-heteroarylidene-1-indanone derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. These compounds are structurally related ...
    • 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 ...
    • 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 ...
    • The design and evaluation of an l-dopa-lazabemide prodrug for the treatment of Parkinson’s disease 

      Hoon, Monique; Petzer, Jacobus P.; Viljoen, Francois; Petzer, Anél (MDPI, 2017)
      l-Dopa, the metabolic precursor of dopamine, is the treatment of choice for the symptomatic relief of the advanced stages of Parkinson’s disease. The oral bioavailability of l-dopa, however, is only about 10% to 30%, and ...
    • The evaluation of 1,4-benzoquinones as inhibitors of human monoamine oxidase 

      Mostert, Samantha; Petzer, Anél; Petzer, Jacobus P. (Elsevier, 2017)
      The monoamine oxidase (MAO) enzymes are of considerable pharmacological interest and inhibitors are used in the clinic for the treatment of major depressive disorder and Parkinson's disease. A limited number of studies ...
    • An evaluation of synthetic indole derivatives as inhibitors of monoamine oxidase 

      Chirkova, Zhanna V.; Petzer, Anél; Petzer, Jacobus P.; Kabanova, Mariya V.; Filimonov, Sergey I. (Elsevier, 2016)
      In a recent study we have shown that several indole-5,6-dicarbonitrile derivatives are potent inhibitors of human monoamine oxidase (MAO) A and B. To expand on these results and to further determine structure–activity ...
    • Inhibition of monoamine oxidase by benzoxathiolone analogues 

      Mostert, Samantha; Petzer, Anél; Petzer, Jacobus P. (Elsevier, 2016)
      Inhibitors of the monoamine oxidase (MAO) enzymes are considered useful therapeutic agents, and are used in the clinic for the treatment of depressive illness and Parkinson’s disease. In addition, MAO inhibitors are also ...
    • Inhibition of monoamine oxidase by indole-5,6-dicarbonitrile derivatives 

      Chirkova, Zhanna V.; Petzer, Anél; Petzer, Jacobus P.; Kabanova, Mariya V.; Filimonov, Sergey I. (Elsevier, 2015)
      Recent studies have found that phthalonitrile derivatives are remarkably potent inhibitors of human monoamine oxidase (MAO) A and B. In an attempt to further determine the structure-activity relationships (SARs) for MAO ...