Browsing Faculty of Health Sciences by Author "10727388 - Petzer, Jacobus Petrus"
Now showing items 1-20 of 97
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1,3,4-Oxadiazol-2-ylbenzenesulfonamides as privileged structures for the inhibition of monoamine oxidase B
Shetnev, Anton; Petzer, Anél; Petzer, Jacobus P.; Shlenev, Roman; Efimova, Julia (Elsevier, 2019)The present study investigates the monoamine oxidase (MAO) inhibition properties of a series of ten 5-aryl-1,3,4-oxadiazol-2-ylbenzenesulfonamides. The target compounds were synthesized by dehydration of the corresponding ... -
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 ... -
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 ... -
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 ... -
8-Aryl- and alkyloxycaffeine analogues as inhibitors of monoamine oxidase
Strydom, Belinda; Bergh, Jacobus J.; Petzer, Jacobus P. (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 ... -
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 ... -
Benzo[b]tiophen-3-ol derivatives as effective inhibitors of human monoamine oxidase: design, synthesis, and biological activity
Guglielmi, Paolo; Petzer, Anél; Petzer, Jacobus P.; Secci, Danela; Bagetta, Donatella (Taylor & Francis, 2019)A series of benzo[b]thiophen-3-ols were synthesised and investigated as potential human monoamine oxidase (hMAO) inhibitors in vitro as well as ex vivo in rat cortex synaptosomes by means of evaluation of 3,4-dihydroxyphenylacetic ... -
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 ...