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Browsing by Author "Egan, Timothy J."

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Multistage antiplasmodium activity of astemizole analogues and inhibition of hemozoin formation as a contributor to their mode of action

Kumar, Malkeet; Okombo, John; Mambwe, Dickson; Taylor, Dale; Lawrence, Nina; Reader, Janette; Van der Watt, Mariette Elizabeth; Fontinha, Diana; Sanches-Vaz, Margarida; Bezuidenhout, Belinda C.; Lauterbach, Sonja B.; Liebenberg, Dale; Birkholtz, Lyn-Marie; Coetzer, Theresa L.; Prudêncio, Miguel; Egan, Timothy J.; Wittlin, Sergio; Chibale, Kelly (American Chemical Society, 2019-02)

A drug repositioning approach was leveraged to derivatize astemizole (AST), an antihistamine drug whose antimalarial activity was previously identified in a high-throughput screen. The multistage activity potential against ...
Naphthylisoquinoline alkaloids, validated as hit multistage antiplasmodial natural products

Moyo, Phanankosi; Shamburger, William; Van der Watt, Mariette Elizabeth; Reader, Janette; De Sousa, Ana Carolina C.; Egan, Timothy J.; Maharaj, Vinesh J.; Bringmann, Gerhard; Birkholtz, Lyn-Marie (Elsevier, 2020-08)

The discovery and development of multistage antimalarial drugs targeting intra-erythrocytic asexual and sexual Plasmodium falciparum parasites is of utmost importance to achieve the ambitious goal of malaria elimination. Here, ...
Novel 3-trifluoromethyl-1,2,4-oxadiazole analogues of astemizole with multi-stage antiplasmodium activity and in vivo efficacy in a Plasmodium berghei mouse malaria infection model

Mambwe, Dickson; Korkor, Constance M.; Mabhula, Amanda; Ngqumba, Zama; Cloete, Cleavon; Kumar, Malkeet; Barros, Paula Ladeia; Leshabane, Meta Kgaogelo; Coertzen, Dina; Taylor, Dale; Gibhard, Liezl; Njoroge, Mathew; Lawrence, Nina; Reader, Janette; Moreira, Diogo Rodrigo; Birkholtz, Lyn-Marie; Wittlin, Sergio; Egan, Timothy J.; Chibale, Kelly (American Chemical Society, 2022-12)

Please read abstract in the article.
Structure-activity relationship studies and Plasmodium life cycle profiling identifies pan-active N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazoles which are efficacious in an in vivo mouse model of malaria

Mayoka, Godfrey; Njoroge, Mathew; Okombo, John; Gibhard, Liezl; Sanches-Vaz, Margarida; Fontinha, Diana; Birkholtz, Lyn-Marie; Reader, Janette; Van der Watt, Mariette Elizabeth; Coetzer, Theresa L.; Lauterbach, Sonja B.; Churchyard, Alisje; Bezuidenhout, Belinda C.; Egan, Timothy J.; Yeates, Clive Leonard; Wittlin, Sergio; Prudêncio, Miguel; Chibale, Kelly (American Chemical Society, 2019)

Structure–activity relationship studies involving N-aryl-3-trifluoromethyl pyrido[1,2-a]benzimidazoles (PBI) identified several compounds possessing potent in vitro activities against the asexual blood, liver, and gametocyte ...

Browsing by Author "Egan, Timothy J."

Browsing by Author "Egan, Timothy J."

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