Browsing Research Output by Author "12902608 - Legoabe, Lesetja Jan"
Now showing items 1-20 of 35
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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-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 ... -
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 ... -
5-Substituted 2-benzylidene-1-tetralone analogues as A1 and/or A2A antagonists for the potential treatment of neurological conditions
Janse van Rensburg, H.D.; Terre'Blanche, G.; Van der Walt, M.M.; Legoabe, L.J. (Elsevier, 2017)Adenosine A1 and A2A receptors are attracting great interest as drug targets for their role in cognitive and motor deficits, respectively. Antagonism of both these adenosine receptors may offer therapeutic benefits in ... -
6-Nitro-1-benzylquinolones exhibiting specific antitubercular activity
Beteck, Richard M.; Van der Kooy, Frank; Legoabe, Lesetja J.; Jordaan, Audrey; Swart, Tarryn (Wiley, 2020)In this study, we synthesized novel nitro quinolone‐based compounds and tested them in vitro against a panel of Gram‐positive and Gram‐negative pathogens including Mycobacterium tuberculosis (MTB), Pseudomonas aeruginosa ... -
Anti-trypanosomal and antimalarial properties of tetralone derivatives and structurally related benzocycloalkanones
Beteck, Richard M.; Legoabe, Lesetja J.; Isaacs, Michelle; Khanye, Setshaba D.; Laming, Dustin (MDPI, 2019)Background and objectives: Sleeping sickness and malaria alike are insect-borne protozoan diseases that share overlapping endemic areas in sub-Saharan Africa. The causative agent for malaria has developed resistance ... -
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 ... -
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 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 ... -
In vitro anti-trypanosomal activities of indanone-based chalcones
Beteck, Richard M.; Legoabe, Lesetja J.; Isaacs, Michelle; Hoppe, Heinrich C. (Thieme, 2019)Human African trypanosomiasis is a neglected infectious disease that affects mostly people living in the rural areas of Africa. Current treatment options are limited to just four drugs that have been in use of four to nine ... -
In-vitro transdermal penetration of cytarabine and its N4-alkylamide derivatives
Legoabe, Lesetja J.; Breytenbach, Jaco C.; N'Da, David D.; Breytenbach, J. Wilma (Wiley, 2010)Objectives The aim of this study was to synthesise and determine the transdermal penetration of cytarabine alkylamide derivatives and assess the correlation of flux with physicochemical properties. Methods The alkylamide ... -
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 ... -
Methoxy substituted 2-benzylidene-1-indanone derivatives as A1 and/or A2A AR antagonists for the potential treatment of neurological conditions
Janse van Rensburg, Helena D.; Legoabe, Lesetja J.; Terre'Blanche, Gisella; Van der Walt, Mietha M. (RSC, 2019)A prior study reported on hydroxy substituted 2-benzylidene-1-indanone derivatives as A1 and/or A2A antagonists for the potential treatment of neurological conditions. A lead compound (1a) was identified with both A1 and ... -
Metronidazole-conjugates: a comprehensive review of recent developments towards synthesis and medicinal perspective
Patel, Om P.S.; Jesumoroti, Omobolanle Janet; Legoabe, Lesetja J.; Beteck, Richard M. (Elsevier, 2020)Nitroimidazoles based compounds remain a hot topic of research in medicinal chemistry due to their numerous biological activities. Moreover, many clinical candidates based on this chemical core have been reported to be ... -
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 ... -
The monoamine oxidase inhibition properties of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives
Marais, Lereze; Petzer, Anél; Petzer, Jacobus P.; Legoabe, Lesetja J. (Springer, 2020)Quinazolinone compounds are of interest in medicinal chemistry since they display a wide range of biological properties. In the present study, a series of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one ... -
The monoamine oxidase inhibition properties of C6-mono- and N3/C6-disubstituted derivatives of 4(3H)-quinazolinone
Qhobosheane, Malikotsi A.; Legoabe, Lesetja J.; Petzer, Anél; Petzer, Jacobus P. (Elsevier, 2019)Parkinson’s disease is characterised by the death of the nigrostriatal neurons and depletion of striatal dopamine. The standard symptomatic therapy consists of dopamine replacement with l-dopa, the metabolic precursor of ... -
Quinolone-isoniazid hybrids: synthesis and preliminary in vitro cytotoxicity and anti-tuberculosis evaluation
Beteck, Richard M.; Legoabe, Lesetja J.; Seldon, Ronnett; Jordaanc, Audrey; Warner, Digby F. (RSC, 2019)Herein, we propose novel quinolones incorporating an INH moiety as potential drug templates against TB. The quinolone-based compounds bearing an INH moiety attached via a hydrazide–hydrazone bond were synthesised and ...