Browsing by Author "Qhobosheane, Malikotsi A."
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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 ... -
Synthesis and evaluation of 2-substituted 4(3H)-quinazolinone thioether derivatives as monoamine oxidase inhibitors
Qhobosheane, Malikotsi A.; Petzer, Anél; Petzer, Jacobus P.; Legoabe, Lesetja J. (Elsevier, 2018)In the present study, a series of fourteen 2-mercapto-4(3H)-quinazolinone derivatives was synthesised and evaluated as potential inhibitors of the human monoamine oxidase (MAO) enzymes. Quinazolinone is the oxidised form ... -
Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors
Qhobosheane, Malikotsi A.; Legoabe, Lesetja J.; Petzer, Jacobus P.; Beteck, Richard M.; Josselin, Béatrice (Elsevier, 2020)Protein kinases are important drug targets, especially in the area of oncology. This paper reports the synthesis and biological evaluation of new 7-azaindole derivatives bearing benzocycloalkanone motifs as potential protein ... -
Synthesis and evaluation of C3 substituted chalcone-based derivatives of 7-azaindole as protein kinase inhibitors
Qhobosheane, Malikotsi A.; Legoabe, Lesetja J.; Beteck, Richard M.; Josselin, Béatrice; Bach, Stéphane (Wiley, 2020)Chalcones are a group of naturally occurring or synthetic compounds which possess a wide range of biological activities. In this paper, a series of twenty‐three 7‐azaindole‐chalcone hybrids (5a–w) were synthesized and ...