Browsing Research Output by Author "Terre'Blanche, Gisella"
Now showing items 1-20 of 25
-
1,3,7-Triethyl-substituted xanthines-possess nanomolar affinity for the adenosine A1 receptor
Van der Walt, Mietha M.; Terre'Blanche, Gisella (Elsevier, 2015)Adenosine A1 receptors are attracting great interest as drug targets for their role in cognitive deficits. Antagonism of the adenosine A1 receptor may offer therapeutic benefits in complex neurological diseases, such as ... -
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 analogues as dual adenosine A1/A2a receptor antagonists for the potential treatment of neurological conditions
Janse van Rensburg, Helena Dorothea; Legoabe, Lesetja J.; Terre'Blanche, Gisella; Van der Walt, Mietha M. (Thieme, 2019)Previous studies explored 2-benzylidine-1-tetralone derivatives as innovative adenosine A1 and A2A receptor antagonists for alternative non-dopaminergic treatment of Parkinson’s disease. This study’s aim is to investigate ... -
8-(3-phenylpropyl)-1,3,7-triethylxanthine is a synthetic caffeine substitute with stronger metabolic modulator activity
Carrageta, David F.; Van der Walt, Mietha M.; Terre'Blanche, Gisella; Dias, Tânia R.; Jarak, Ivana (Elsevier, 2018)Caffeine is one of the most worldwide consumed methylxanthines. It is well-known for its thermogenic and cell metabolism modulating effects. Based on methylxanthines' chemical structure, 8-(3-phenylpropyl)-1,3,7-triethylxanthine ... -
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- ... -
Benzopyrone represents a privilege scaffold to identify novel adenosine A1/A2A receptor antagonists
Van der Walt, Mietha M.; Terre'Blanche, Gisella (Elsevier, 2018)Adenosine receptor antagonists are under investigation as potential drug candidates for the treatment of certain cancers, neurological disorders, depression and potentially improve tumour immunotherapy. The benzo-γ-pyrone ... -
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 ... -
C2-substituted quinazolinone derivatives exhibit A1 and/or A2A adenosine receptor affinities in the low micromolar range
Pieterse, Lianie; Van der Walt, Mietha M.; Terre'Blanche, Gisella (Elsevier, 2020)Antagonists of the adenosine receptors (A1 and A2A subtypes) are widely researched as potential drug candidates for their role in Parkinson’s disease-related cognitive deficits (A1 subtype), motor dysfunction (A2A subtype) ... -
C3 amino-substituted chalcone derivative with selective adenosine rA1 receptor affinity in the micromolar range
Janse van Rensburg, Helena D.; Legoabe, Lesetja J.; Terre'Blanche, Gisella (Springer, 2020)To identify novel adenosine receptor (AR) ligands based on the chalcone scaffold, herein the synthesis, characterization and in vitro and in silico evaluation of 33 chalcones (15–36 and 37–41) and structurally related ... -
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, ... -
Deuterium isotope effects for the oxidation of 1-methyl-3phenyl-3pyrrolinyl analogues by monoamine oxidase B
Pretorius, Anél; Ogunrombi, Modupe O.; Terre'Blanche, Gisella; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2008)The parkinsonian inducing agent, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), is a cyclic tertiary allylamine exhibiting good monoamine oxidase B (MAO-B) substrate properties. MAO-B catalyzes the ring α-carbon ... -
Die adenosien A1- en A2A-reseptoraffiniteit van ’n reeks 3,4-dihidropirimidoon-analoë
Katsidzira, Runako M.; Van der Walt, Mietha M.; Bergh, Jacobus J.; Terre'Blanche, Gisella (AOSIS, 2017)Parkinson se siekte is ’n komplekse neurodegeneratiewe siektetoestand. Huidige behandeling van dié siekte is slegs op simptomatiese verligting gemik, sonder dat die siekteverloop vertraag of gestop word. Sedert die ... -
Die identifisering van fenielbottersuur aromatiese metaboliete in die urien van die blou-aap
Van der Linde, Wilhelmina J.; Mienie, Lodewyk J.; Bergh, Jacobus J.; Van der Walt, Mietha M.; Terre'Blanche, Gisella (Suid-Afrikaanse Akademie vir Wetenskap en Kuns, 2018)Phenylbutyrate (PBA) is used as treatment of urea cycle disorders and as an alternative treatment option for adrenoleykodystrophy, has neuroprotective effects and provides protection against oxidative stress. Known ... -
Discovery of 1,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine derivatives as novel adenosine A1 and A2A receptor antagonists
Harmse, Rozanne; Van der Walt, Mietha M.; Petzer, Jacobus P.; Terre'Blanche, Gisella (Elsevier, 2016)Based on a previous report that a series of 8-(phenoxymethyl)-xanthines may be promising leads for the design of A1 adenosine receptor antagonists, selected novel and known 1,3-diethyl-7-methyl-8-(phenoxymethyl)-xanthine ... -
Evaluation of 2-benzylidene-1-tetralone derivatives as antagonists of A1 and A2A adenosine receptors
Legoabe, Lesetja J.; Van der Walt, Mietha M.; Terre'Blanche, Gisella (Wiley, 2018)Antagonists of the adenosine receptors (A1 and A2A) are thought to be beneficial in neurological disorders, such as Alzheimer's and Parkinson's disease. The aim of this study was to explore 2-benzylidene-1-tetralone ... -
Imidazo[1,2-α]pyridines possess adenosine A1 receptor affinity for the potential treatment of cognition in neurological disorders
Lefin, Roslyn; Van der Walt, Mietha M.; Milne, Pieter J.; Terre'Blanche, Gisella (Elsevier, 2017)Previous research has shown that bicyclic 6:5-fused heteroaromatic compounds with two N-atoms have variable degrees of adenosine A1 receptor antagonistic activity. Prompted by this imidazo[1,2-α]pyridine analogues were ... -
Novel sulfanylphthalimide analogues as highly potent inhibitors of monoamine oxidase B
Van der Walt, Mietha M.; Terre'Blanche, Gisella; Petzer, Anél; Petzer, Jacobus P. (Elsevier, 2012)Monoamine oxidase (MAO) plays an essential role in the catabolism of neurotransmitter amines. The two isoforms of this enzyme, MAO-A and -B, are considered to be drug targets for the therapy of depression and neurodegenerative ... -
Paracetamol prevents hyperglycinemia in vervet monkeys treated with valproate
Viljoen, Jacques; Bergh, Jacobus J.; Mienie, Lodewyk J.; Terre'Blanche, Gisella; Kotzé, Herculaas F. (Springer, 2012)Valproate administration increases the level of the inhibitory transmitter, glycine, in the urine and plasma of patients and experimental animals. Nonketotic hyperglycinemia (NKH), an autosomal recessive disorder of ... -
Structure-activity relationships in the inhibition of monoamine oxidase B by 1-methyl-3-phenylpyrroles
Ogunrombi, Modupe O.; Malan, Sarel F.; Terre'Blanche, Gisella; Bergh, Jacobus J.; Petzer, Jacobus P. (Elsevier, 2008)1-Methyl-3-phenyl-3-pyrrolines are structural analogues of the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) and like MPTP are selective substrates of monoamine oxidase B (MAO-B). As part of an ongoing ... -
The styrene metabolite, phenylglyoxylic acid, induces striatal-motor toxicity in the rat: influence of dose escalation/reduction over time
Terre'Blanche, Gisella; Heyer, Nicolette; Bergh, Jacobus J.; Mienie, Lodewyk J.; Harvey, Brian H.; Van der Schyf, Cornelius J. (Springer, 2011)Exposure to the industrial solvent, styrene, induces locomotor and cognitive dysfunction in rats, and parkinsonian-like manifestations in man. The antipsychotic, haloperidol (HP), well known to induce striatal toxicity in ...