Search Results - "Legoabe, Lesetja"

Antimalarial application of quinones: A recent update by Patel, Om P.S., Beteck, Richard M., Legoabe, Lesetja J.

“…Atovaquone belongs to a naphthoquinone class of drugs and is used in combination with proguanil (Malarone) for the treatment of acute, uncomplicated malaria…”
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Quinolone: a versatile therapeutic compound class by Dube, Phelelisiwe S., Legoabe, Lesetja J., Beteck, Richard M.

“…The discovery of nalidixic acid is one pinnacle in medicinal chemistry, which opened a new area of research that has led to the discovery of several…”
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An Update on Development of Small-Molecule Plasmodial Kinase Inhibitors by Moolman, Chantalle, Sluis, Rencia van der, Beteck, Richard M, Legoabe, Lesetja J

“…Malaria control relies heavily on the small number of existing antimalarial drugs. However, recurring antimalarial drug resistance necessitates the continual…”
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Steroid-triazole conjugates: A brief overview of synthesis and their application as anticancer agents by Agarwal, Devesh S., Sakhuja, Rajeev, Beteck, Richard M., Legoabe, Lesetja J.

“…[Display omitted] •Steroids are biomolecules that mediate several vital physiological processes.•Triazole due to their electronic and topological features play…”
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Recent Advances in Radical C−H Bond Functionalization of Imidazoheterocycles by Patel, Om P. S., Nandwana, Nitesh K., Legoabe, Lesetja J., Das, Bhaskar C., Kumar, Anil

“…Direct C−H bond functionalization through radical pathway has emerged as a powerful and ideal strategy for the synthesis of organic compounds. This review…”
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Exploration of artemisinin derivatives and synthetic peroxides in antimalarial drug discovery research by Patel, Om P.S., Beteck, Richard M., Legoabe, Lesetja J.

“…Malaria is a life-threatening infectious disease caused by protozoal parasites belonging to the genus Plasmodium. It caused an estimated 405,000 deaths and 228…”
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Chemical Classes Presenting Novel Antituberculosis Agents Currently in Different Phases of Drug Development: A 2010–2020 Review by Angula, Klaudia T., Legoabe, Lesetja J., Beteck, Richard M.

“…Tuberculosis (TB), caused by Mycobacterium tuberculosis (Mtb), is a curable airborne disease currently treated using a drug regimen consisting of four drugs…”
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The evaluation of N-propargylamine-2-aminotetralin as an inhibitor of monoamine oxidase by Meiring, Letitia, Petzer, Jacobus P., Legoabe, Lesetja J., Petzer, Anél

“…Interestingly, it was found that 2-PAT is a reversible (R) MAO-A inhibitor, while acting as an inactivator (I) of MAO-B. [Display omitted] •2-PAT is an…”
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Quinolone analogues of benzothiazinone: Synthesis, antitubercular structure-activity relationship and ADME profiling by Dube, Phelelisiwe S., Legoabe, Lesetja J., Jordaan, Audrey, Sigauke, Lester, Warner, Digby F., Beteck, Richard M.

“…Mycobacterium tuberculosis (Mtb) has an impermeable cell wall which gives it an inherent ability to resist many antibiotics. DprE1, an essential enzyme in Mtb…”
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Nigella sativa L. and Its Active Compound Thymoquinone in the Clinical Management of Diabetes: A Systematic Review by Mahomoodally, Mohamad Fawzi, Aumeeruddy, Muhammad Zakariyyah, Legoabe, Lesetja J, Montesano, Domenico, Zengin, Gokhan

“…Despite existing conventional hypoglycemic drugs to manage diabetes, their non-availability and cost in low-income countries coupled with the associated side…”
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Exploration of 7-azaindole-coumaranone hybrids and their analogues as protein kinase inhibitors by Qhobosheane, Malikotsi A., Beteck, Richard M., Baratte, Blandine, Robert, Thomas, Ruchaud, Sandrine, Bach, Stéphane, Legoabe, Lesetja J.

“…7-Azaindole has been labelled a privileged scaffold for the design of new potent inhibitors of protein kinases. In this paper, we determined the inhibition…”
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Synthesis and biological evaluation of selected 7H-pyrrolo[2,3-d]pyrimidine derivatives as novel CDK9/CyclinT and Haspin inhibitors by Pieterse, Lianie, Beteck, Richard M., Baratte, Blandine, Jesumoroti, Omobolanle J., Robert, Thomas, Ruchaud, Sandrine, Bach, Stéphane, Legoabe, Lesetja J.

“…Protein kinases, including CDK9/CyclinT and Haspin, are regarded as potential drug targets in cancer therapy. Findings from a previous study suggested…”
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Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective by Patel, Om P.S., Jesumoroti, Omobolanle Janet, Legoabe, Lesetja J., Beteck, Richard M.

“…Nitroimidazoles based compounds remain a hot topic of research in medicinal chemistry due to their numerous biological activities. Moreover, many clinical…”
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Pyrazolyl amide-chalcones conjugates: Synthesis and antikinetoplastid activity by Agarwal, Devesh S, Beteck, Richard M, Mabille, Dorien, Caljon, Guy, Legoabe, Lesetja J

“…A series of novel pyrazolyl amide-chalcones conjugates was synthesized in five steps and evaluated against a range of medically important kinetoplastid…”
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Hydrazinated geraniol derivatives as potential broad‐spectrum antiprotozoal agents by Jooste, Joelien, Legoabe, Lesetja J., Ilbeigi, Kayhan, Caljon, Guy, Beteck, Richard M.

“…Geraniol, a primary component of several essential oils, has been associated with broad‐spectrum antiprotozoal activities, although moderate to weak. This…”
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2-Aroyl quinazolinone: Synthesis and in vitro anti-parasitic activity by Setshedi, Koketso J, Beteck, Richard M, Jesumoroti, Omobolanle J, Ilbeigi, Kayhan, Mabille, Dorien, Caljon, Guy, Van der Kooy, Frank, Legoabe, Lesetja J

“…Trypanosomes and Leishmania are parasitic protozoans that affect millions of people globally. Herein we report the synthesis of 2-aroyl quinazolinones and…”
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α-Tetralone derivatives as inhibitors of monoamine oxidase by Legoabe, Lesetja J., Petzer, Anél, Petzer, Jacobus P.

“…In the present study, a series of fifteen α-tetralone (3,4-dihydro-2H-naphthalen-1-one) derivatives were synthesised and evaluated as inhibitors of recombinant…”
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Synthesis and in vitro antitrypanosomal evaluation of novel 6-heteroarylidene-substituted quinolone derivatives by Angula, Klaudia T., Legoabe, Lesetja J., Swart, Tarryn, Hoppe, Heinrich C., Beteck, Richard M.

“…Human African trypanosomiasis is a vector-borne tropical disease of African origin. Presently, due to human migration and climate change, the disease might…”
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Design and synthesis of imidazo[1,2‐a]pyridine‐chalcone conjugates as antikinetoplastid agents by Agarwal, Devesh S., Beteck, Richard M., Ilbeigi, Kayhan, Caljon, Guy, Legoabe, Lesetja J.

“…A library of imidazo[1,2‐a]pyridine‐appended chalcones were synthesized and characterized using 1H NMR, 13C NMR and HRMS. The synthesized analogues were…”
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Validating a sensitive LCMS method for the quantitation of artemisinin in Artemisia spp. including material used in retracted clinical trials by Lee, Barend J., van Niekerk, Suzanne E., Legoabe, Lesetja J., van der Kooy, Frank

“…•A sensitive LCMS method was developed for the quantitation of artemisinin in Artemisia annua and A. afra.•This method was applied to a collection of Artemisia…”
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