Browsing by Author "Beteck, Richard M."
Now showing items 1-9 of 9
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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 ... -
Accessible and distinct decoquinate derivatives active against Mycobacterium tuberculosis and apicomplexan parasites
Beteck, Richard M.; Smit, Frans J.; N'Da, David D.; Haynes, Richard K.; Seldon, Ronnett (Nature, 2018)The quinolone decoquinate is coadministered with feed for treatment of parasites which cause coccidiosis in poultry. However, from a drug-development perspective, the biological activity is often not adequately exploited ... -
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 ... -
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 ... -
Recent progress in the development of anti-malarial quinolones
Beteck, Richard M.; Smit, Frans J.; Haynes, Richard K.; N'Da, David D. (BioMed Central, 2014)Available anti-malarial tools have over the ten-year period prior to 2012 dramatically reduced the number of fatalities due to malaria from one million to less than six-hundred and thirty thousand. Although fewer people ... -
Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities
Beteck, Richard M.; Smit, Frans J.; Haynes, Richard K.; N'Da, David D.; Coertzen, Dina (Elsevier, 2016)As part of a programme aimed at identifying rational new triple drug combinations for treatment of malaria, tuberculosis and toxoplasmosis, we have selected quinolones as one component, given that selected examples exhibit ... -
Synthesis and biological evaluation of selected 7-azaindole derivatives as CDK9/Cyclin T and Haspin inhibitors
Pieterse, Lianie; Legoabe, Lesetja J.; Beteck, Richard M.; Josselin, Béatrice; Bach, Stéphane (Springer, 2020)The 7-azaindole scaffold attracts attention due to its value in the design of inhibitors of diseases related protein kinases. However, this scaffold has not been evaluated against Haploid germ cell-specific nuclear protein ... -
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 ...