Browsing Faculty of Health Sciences by Author "10199667 - Malan, Sarel Francois"
Now showing items 1-20 of 21
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Antioxidant properties of 4-quinolones and structurally related flavones
Greeff, Jane; Van Dyk, Sandra; Malan, Sarel F.; Joubert, Jacques (Elsevier, 2012)Neurodegenerative disorders are frequently associated with increased oxidative damage to the brain as a result of free radicals produced by cellular respiration. The onset and progression of neurodegeneration may therefore ... -
Crystal structure of a rearranged cage compound 3-hydroxy-4-aza-8-oxoheptacyclo [9.4.1.0-2,10-, 0 -3,14-, 0-4,9-, 0-9,13-, 0-12,12]tetradecane
Prins, Louis H.A.; De Vries, Armand; Oliver, Douglas W.; Van Dyk, Sandra; Malan, Sarel F. (Springer, 2008)Polycyclic hydrocarbon compounds exhibit a wide variety of biological activities, ranging from antiviral to Parkinson’s disease. Several structures such as the adamantanes have reached clinical status and are used ... -
Dual inhibition of monoamine oxidase B and antagonism of the adenosine A2A receptor by (E,E)-8-(4phenylbytadien-1-yl) caffeine analogues
Malan, Sarel F.; Bergh, Jacobus J.; Petzer, Jacobus P.; Castagnoli, Neal; Pretorius, Judey (Elsevier, 2008)The adenosine A2A receptor has emerged as an attractive target for the treatment of Parkinson’s disease (PD). Evidence suggests that antagonists of the A2A receptor (A2A antagonists) may be neuroprotective and may help to ... -
Fluorescent polycyclic ligands for nitric oxide synthase (NOS) inhibition
Joubert, Jacques; Van Dyk, Sandra; Malan, Sarel F. (Elsevier, 2008)In recent years polycyclic compounds have been shown to exhibit pharmacological profiles of importance in the symptomatic and proposed curative treatment of neurodegenerative diseases (e.g., Parkinson’s and Alzheimer’s ... -
The high performance liquid chromatography (HPLC) analysis of ultraviolet (UV) irradiated chlorophyll a and secondary plant compounds
Scheepers, Johanna C.; Malan, Sarel F.; Du Preez, Jan L.; Van Dyk, Sandra (Academic Journals, 2011)A large number of diseases such as cancer, cardiovascular disease, inflammatory disease, neurodegenerative disorders and ageing are consequences of reactive oxygen species (ROS) and reactive nitrogen species (RNS). ... -
The importance of including toxicity assays when screening plant extracts for antimalarial activity
Van Dyk, Sandra; Griffiths, Sharon; Malan, Sarel F.; Van Zyl, Robyn L. (Academic Journals, 2009)Identifying plant extracts as sources of antimalarial compounds needs to be addressed as numerous studies screen extracts without the means of eliminating extracts that are merely cytotoxic. Fifty-nine organic solvent ... -
Inhibition of monoamine oxidase by 8-benzyloxycaffeine analogues
Strydom, Belinda; Malan, Sarel F.; Bergh, Jacobus J.; Petzer, Jacobus P.; Castagnoli, Neal (Elsevier, 2010)Based on recent reports that several (E)-8-styrylcaffeinyl analogues are potent reversible inhibitors of monoamine oxidase B (MAO-B), a series of 8-benzyloxycaffeinyl analogues were synthesized and evaluated as inhibitors ... -
Inhibition of monoamine oxidase by E-styrylisatin analogues
Van der Walt, Elizna M.; Bergh, Jacobus J.; Petzer, Jacobus P.; Malan, Sarel F.; Milczek, E.M. (Elsevier, 2009)Previous studies have shown that (E)-8-(3-chlorostyryl)caffeine (CSC) is a specific reversible inhibitor of human monoamine oxidase B (MAO-B) and does not bind to human MAO-A. Since the small molecule isatin is a natural ... -
Inhibition of monoamine oxidase by indole and benzofuran derivatives
Prins, Louis H.A.; Petzer, Jacobus P.; Malan, Sarel F. (Elsevier, 2010)Monoamine oxidase (MAO) is an important drug target for the treatment of neurological disorders. A series of indole and benzofuran derivatives were synthesised and evaluated as inhibitors of the two MAO isoforms, MAO-A and ... -
Inhibition of monoamine oxidase by 8-benzyloxycaffeine analogues
Strydom, Belinda; Malan, Sarel F.; Bergh, Jacobus J.; Petzer, Jacobus P.; Castagnoli, Neal (Elsevier, 2010)Based on recent reports that several (E)-8-styrylcaffeinyl analogues are potent reversible inhibitors of monoamine oxidase B (MAO-B), a series of 8-benzyloxycaffeinyl analogues were synthesized and evaluated as inhibitors ... -
Medicinal chemistry of polycyclic cage compounds in drug discovery research
Oliver, Douglas W.; Malan, Sarel F. (Springer, 2008)Saturated polycyclic hydrocarbon structures such as the monocyclic octane, bicylic norbornane and tricyclic adamantane have attracted the attention of several research groups since the 1930s. In the 1950s the synthesis of ... -
Nitric oxide syntase inhibition by pentacycloundecane conjugates of aminoguanidine and tryptamine
Wilkes, Dennis K.; De Vries, Armand; Oliver, Douglas W.; Malan, Sarel F. (Wiley, 2009)This paper describes the synthesis and in-vitro activity of pentacycloundecane-conjugated aminoguanidine and tryptamine analogues on nitric oxide synthase (NOS) using rat brain homogenate. Both aminoguanidine and ... -
Polycyclic cage structures as carrier molecules for neuroprotective non-steroidal anti-inflammatory drugs
Du Preez, Jan L.; Van Dyk, Sandra; Malan, Sarel F. (Elsevier, 2009)The blood-brain barrier is formed by the brain capillary endothelium and plays the predominant role in controlling the passage of substances between the blood and the brain. Recent studies on polycyclic structures, i.e. ... -
Polycyclic propargylamine and acetylene derivatives as multifunctional neuroprotective agents
Zindo, Frank T.; Barber, Quinton R.; Bergh, Jacobus J.; Petzer, Jacobus P.; Malan, Sarel F. (Elsevier, 2014)The aim of this study was to design drug-like molecules with multiple neuroprotective mechanisms which would ultimately inhibit N-methyl-D-aspartate (NMDA) receptors, block L-type voltage gated calcium channels (VGCC) ... -
Role of monoamine oxidase, nitric oxide synthase and regional brain monoamines in the antidepressant-like effects of methylene blue and selected structural analogues
Harvey, Brian H.; Duvenhage, Ingrid; Viljoen, Francois; Scheepers, Nellie; Brink, Christiaan B.; Petzer, Jacobus P.; Malan, Sarel F. (Elsevier, 2010)Dual action antidepressants have important therapeutic implications. Methylene blue (MB), a charged compound structurally related to tricyclic antidepressants, acts on both monoamine oxidase (MAO) and the nitric oxide ... -
S-nitrosylation and attenuation of excessive calcium flux by pentacycloundecane derivatives
Lemmer, Hendrik J.R.; Joubert, Jacques; Van Dyk, Sandra; Van der Westhuizen, Francois H.; Malan, Sarel F. (Bentham Science, 2012)A novel series of polycyclic amines, containing nitrogen monoxide donating moieties, were synthesised and tested for calcium channel and N-methyl-D-aspartate receptor modulating activity. The synthesised compounds were ... -
Small molecule fluorescent ligands as central nervous system imaging probes
Joubert, Jacques; Van Dyk, Sandra; Malan, Sarel F. (Bentham Science, 2013)The design, development and use of small molecule fluorescent ligands to directly or indirectly study receptors, enzymes and other targets in the central nervous system (CNS) have in the recent years become an intense area ... -
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 ... -
Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents
Joubert, Jacques; Van Dyk, Sandra; Malan, Sarel F.; Green, Ivan R. (Elsevier, 2011)A series of fluorescent heterocyclic adamantane amines were synthesised with the goal to develop novel fluorescent ligands for neurological assay development. These derivatives demonstrated multifunctional neuroprotective ... -
Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxice synthase inhibitors
Prins, Louis H.A.; Petzer, Jacobus P.; Malan, Sarel F. (Elsevier, 2009)Monoamine oxidase B (MAO-B) and nitric oxide synthase (NOS) have both been implicated in the pathology of neurodegenerative diseases. In an attempt to design dual-target-directed drugs that inhibit both these enzymes, a ...