Browsing Faculty of Health Sciences by Author "cb2c72d5-97f1-43dc-bf5a-4fb4f2668fc7"
Now showing items 1-6 of 6
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11-Azaartemisinin cocrystals with preserved lactam : acid heterosynthons
Nisar, Madiha; Haynes, Richard K.; Sung, Herman H.-Y.; Puschmann, Horst; Lakerveld, Richard (RSC, 2018)11-Azaartemisinin (11-Aza) is a potent anti-malarial drug more readily able to form cocrystals than its parent compound. 13 new 1 : 1 and 2 : 1 cocrystal phases from 25 mono- and bi-functional acids are reported here in ... -
Cocrystals of the antimalarial drug 11-azaartemisinin with three alkenoic acids of 1:1 or 2:1 stoichiometry
Nisar, Madiha; Haynes, Richard K.; Wong, Lawrence W.; Sung, Herman H.-Y.; Williams, Ian D. (IUCr, 2018)The stoichiometry, X-ray structures and stability of four pharmaceutical cocrystals previously identified from liquid-assisted grinding (LAG) of 11-azaartemisinin (11-Aza; systematic name: 1,5,9-trimethyl-14,15,16-triox ... -
The evaluation of the anti‐cancer drug elesclomol that forms a redox‐active copper chelate as a potential anti‐tubercular drug
Ngwane, Andile H.; Wong, Ho Ning; Haynes, Richard K.; Petersen, Ray-Dean; Baker, Bienyameen (Wiley, 2019)The observations that the innate immune system employs copper toeliminate bacterial infection and that resistance to copper enhancesvirulence ofMycobacterium tuberculosis(Mtb) prompted us to exam-ine the effects the ... -
An in vitro ADME and in vivo pharmacokinetic study of novel TB-active decoquinate derivatives
Tanner, Lloyd; Haynes, Richard K.; Wiesner, Lubbe (Frontiers Media, 2019)Tuberculosis (TB) is currently the leading cause of mortality due to an infectious disease, despite the existence of multiple effective first-line and second-line drugs. The current anti-TB regimen requires a prolonged ... -
Preliminary evaluation of artemisinin-cholesterol conjugates as potential drugs for the treatment of intractable forms of malaria and tuberculosis
Morake, Mokhitli; Wentzel, Johannes F.; Wong, Ho Ning; Smit, Frans J.; N'Da, David D.; Haynes, Richard K. (Wiley, 2018)To evaluate the feasibility of developing drugs that may be active against both malaria and tuberculosis (TB) by using in part putative cholesterol transporters in the causative pathogens and through enhancement of passive ... -
Topical delivery of artemisone, clofazimine and decoquinate encapsulated in vesicles and their in vitro efficacy against Mycobacterium tuberculosis
Van Zyl, Lindi; Viljoen, Joe M.; Haynes, Richard k.; Aucamp, Marique; Du Plessis, Jeanetta (Springer, 2019)Vesicles are widely investigated as carrier systems for active pharmaceutical ingredients (APIs). For topical delivery, they are especially effective since they create a “depot-effect” thereby concentrating the APIs in the ...