Browsing Research Output by Author "Petzer, Anél"
Now showing items 21-40 of 62
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Exploring 4-substituted-2-thiazolylhydrazones from 2-, 3-, and 4-acetylpyridine as selective and reversible hMAO-B inhibitors
Chimenti, Paola; Petzer, Anél; Petzer, Jacobus P.; Carradori, Simone; D’Ascenzio, Melissa (Elsevier, 2013)A series of 4-substituted-2-thiazolylhydrazone derivatives have been synthesized and tested in vitro for their human monoamine oxidase (hMAO) A and B inhibitory activity. Our findings confirmed that the substitution at ... -
Indanones as high-potency reversible inhibitors of monoamine oxidase
Mostert, Samantha; Petzer, Anél; Petzer, Jacobus P. (Wiley, 2015)Recent reports document that α-tetralone (3,4-dihydro-2H-naphthalen-1-one) is an appropriate scaffold for the design of high-potency monoamine oxidase (MAO) inhibitors. Based on the structural similarity between α-tetralone ... -
Inhibition of human monoamine oxidase: biological and molecular modeling studies on selected natural flavonoids
Carradori, Simone; Petzer, Anél; Petzer, Jacobus P.; Gidaro, Maria Concetta; Costa, Giosuè (ACS, 2016)Naturally occurring flavonoids display a plethora of different biological activities, but emerging evidence suggests that this class of compounds may also act as antidepressant agents endowed with multiple mechanisms of ... -
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 ... -
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 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 ... -
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 ... -
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 ... -
The interactions of azure B, a metabolite of methylene blue, with 2 acetylcholinesterase and butyrylcholinesterase
Petzer, Anél; Harvey, Brian H.; Petzer, Jacobus P. (Elsevier, 2014)Methylene blue(MB) is reported to possess diverse pharmacological actions and is attracting increasing attention for the treatment of neurodegenerative disorders such as Alzheimer's disease. Among the pharmacological actions ... -
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 ... -
Investigation of the monoamine oxidase inhibition properties of benzoxathiolone derivatives
Prinsloo1, Izak F.; Petzer, Anél; Cloete, Theunis T.; Petzer, Jacobus P. (Springer, 2023)The treatment of neuropsychiatric and neurodegenerative disorders such as depression and Parkinson’s disease represent significant challenges in healthcare. Enzymes that metabolise neurotransmitter amines are important ... -
An investigation of the monoamine oxidase inhibition properties of pyrrolo[3,4‐f]indole‐5,7‐dione and indole‐5,6‐dicarbonitrile derivatives
Chirkova, Zhanna, V.; Petzer, Anél; Engelbrecht, Idalet; Petzer, Jacobus P.; Kabanova, Mariya V. (Wiley, 2018)In recent studies, we have shown that pyrrolo[3,4‐f]indole‐5,7‐dione and indole‐5,6‐dicarbonitrile derivatives act as good potency in vitro inhibitors of the monoamine oxidase (MAO) enzymes. To expand on these series and ... -
Kaempferol as selective human MAO‑A inhibitor: analytical detection in Calabrian red wines, biological and molecular modeling studies
Gidaro, Maria Concetta; Petzer, Anél; Petzer, Jacobus P.; Astorino, Christian; Carradori, Simone (ACS, 2016)The purpose of this work was to determine the kaempferol content in three red wines of Calabria, a southern Italian region with a great number of certified food products. Considering that wine cultivar, climate, and soil ... -
Leflunomide, a reversible monoamine oxidase inhibitor
Petzer, Jacobus P.; Petzer, Anél (Bentham Science, 2016)A screening study aimed at identifying inhibitors of the enzyme, monoamine oxidase (MAO), among clinically used drugs have indicated that the antirheumatic drug, leflunomide, is an inhibitor of both MAO isoforms. Leflunomide ... -
Methylene blue analogues with marginal monoamine oxidase inhibition retain antidepressant-like activity
Delport, Anzelle; Harvey, Brian H.; Petzer, Anél; Petzer, Jacobus P. (ACS, 2018)Methylene blue (MB) possesses diverse medical applications. Among these, MB presents with antidepressant-like effects in animals and has shown promise in clinical trials for the treatment of mood disorders. As an antidepressant, ... -
Methylene blue analogues: in vitro antimicrobial minimum inhibitory concentrations and in silico pharmacophore modelling
Thesnaar, Louis; Bezuidenhout, Jaco J.; Petzer, Anél; Petzer, Jacobus P.; Cloete, Theunis T. (Elsevier, 2020)It has been shown that methylene blue has antimicrobial properties although few studies have determined its minimum inhibitory concentration (MIC), which is the gold standard used to measure antimicrobial activity. The ... -
Methylene blue and its analogues as antidepressant compounds
Delport, Anzelle; Harvey, Brian H.; Petzer, Anél; Petzer, Jacobus P. (Springer, 2017)Methylene Blue (MB) is considered to have diverse medical applications and is a well-described treatment for methemoglobinemias and ifosfamide-induced encephalopathy. In recent years the focus has shifted to MB as an ... -
Monoamine oxidase inhibition by selected anilide derivatives
Legoabe, Lesetja; Kruger, Johann; Petzer, Anél; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2011)A series of anilide derivatives were synthesized and evaluated as inhibitors of recombinant human monoamine oxidase (MAO) A and B. The most potent inhibitors among the derivatives that were initially evaluated were ...