Browsing Faculty of Health Sciences by Author "Petzer, Anél"
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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-Aminopyrimidines as dual adenosine A1/A2A antagonists
Robinson, Sarel J.; Petzer, Jacobus P.; Terre'Blanche, Gisella; Petzer, Anél; Van der Walt, Mietha M.; Bergh, Jacobus J.; Lourens, Anna C.U. (Elsevier, 2015)In this study thirteen 2-aminopyrimidine derivatives were synthesised and screened as potential antagonists of adenosine A1 and A2A receptors in order to further investigate the structure activity relationships of this ... -
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 ... -
4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis
Secci, Daniela; Petzer, Anél; Petzer, Jacobus P.; Carradori, Simone; Guglielmi, Paulo (Taylor & Francis, 2019)A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted ... -
The adenosine A2A antagonistic properties of selected C8-substituted xanthines
Van der Walt, Mietha M.; Terre’Blanche, Gisella; Petzer, Anél; Lourens, Anna C.U.; Petzer, Jacobus P. (Elsevier, 2013)The adenosine A2A receptor is considered to be an important target for the development of new therapies for Parkinson’s disease. Several antagonists of the A2A receptor have entered clinical trials for this purpose and ... -
The adenosine receptor affinities and monoamine oxidase B inhibitory properties of sulfanylphthalimide analogues
Van der Walt, Mietha M.; Terre'Blanche, Gisella; Petzer, Anél; Petzer, Jacobus P. (Elsevier, 2015)Based on a report that sulfanylphthalimides are highly potent monoamine oxidase (MAO) B selective inhibitors, the present study examines the adenosine receptor affinities and MAO-B inhibitory properties of a series of 4- ... -
Azure B and a synthetic structural analogue of methylene blue, ethylthioninium chloride, present with antidepressant-like properties
Delport, Anzelle; Harvey, Brian H.; Petzer, Anél; Petzer, Jacobus P. (Elsevier, 2014)Aims: The phenothiazinium compound, methylene blue (MB), possesses diverse pharmacological actions and is attracting attention for the treatment of bipolar disorder and Alzheimer's disease. MB acts on both monoamine oxidase ... -
Azure B, a metabolite of methylene blue, is a high-potency, reversible inhibitor of monoamine oxidase
Petzer, Anél; Harvey, Brian H.; Petzer, Jacobus P.; Wegener, Gregers (Elsevier, 2012)Methylene blue (MB) has been shown to act at multiple cellular and molecular targets and as a result possesses diverse medical applications. Among these is a high potency reversible inhibition of monoamine oxidase A ... -
Benzyloxynitrostyrene analogues: a novel class of selective and highly potent inhibitors of monoamine oxidase B
Van der Walt, Mietha M.; Terre'Blanche, Gisella; Petzer, Jacobus P.; Petzer, Anél (Elsevier, 2017)This study examines a series of novel 3-benzyloxy-β-nitrostyrene analogues as a novel class of inhibitors of the monoamine oxidase (MAO) enzymes. MAO inhibitors are considered useful for the treatment of depression and ... -
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 ... -
Caffeine as a lead compound for the design of therapeutic agents for the treatment of Parkinson’s disease
Petzer, Jacobus P.; Petzer, Anél (Bentham Science, 2015)The current pharmacological therapies for the treatment of Parkinson’s disease are mostly inadequate and recent, improved therapeutic agents are required. Two important molecular targets for the design of anti-parkinsonian ... -
Carbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists
Robinson, Sarel J.; Petzer, Jacobus P.; Terre'Blanche, Gisella; Petzer, Anél; Lourens, Anna C.U.; Rousseau, Amanda L. (Elsevier, 2016)A novel series of carbamate substituted 2-amino-4,6-diphenylpyrimidines was evaluated as potential dual adenosine A1 and A2A receptor antagonists. The majority of the synthesised compounds exhibited promising dual affinities, ... -
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 ... -
Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents
Carradori, Simone; Petzer, Anél; Petzer, Jacobus P.; Ortuso, Francesco; Bagetta, Donatella (Elsevier, 2018)New 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives are proposed as dual-target-directed monoamine oxidase B (MAO-B) and acetylcholinesterase (AChE) inhibitors, as well as antioxidant agents, for the treatment of ... -
Design, synthesis and evaluation of 3-hydroxypyridin-4-ones as inhibitors of catechol-O-methyltransferase
De Beer, Johannie; Petzer, Jacobus P.; Lourens, Anna C.U.; Petzer, Anél (Springer, 2020)The most effective treatment of Parkinson’s disease is restoring central dopamine levels with levodopa, the metabolic precursor of dopamine. However, due to extensive peripheral metabolism by aromatic L-amino acid decarboxylase ... -
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 ... -
The evaluation of 1-tetralone and 4-chromanone derivatives as inhibitors of monoamine oxidase
Cloete, Stephanus J.; N'Da, Clarina I.; Legoabe, Lesetja J.; Petzer, Anél; Petzer, Jacobus P. (Springer, 2020)Monoamine oxidase (MAO) is of much clinical relevance, and inhibitors of this enzyme are used in the treatment for neuropsychiatric and neurodegenerative disorders such as depression and Parkinson’s disease. The present ... -
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 ... -
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 ...