Browsing by Author "20926588 - Smit, Frans Johannes"
Now showing items 1-18 of 18
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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 ... -
Activities of 11-azaartemisinin and N-sulfonyl derivatives against asexual and transmissible malaria parasites
Harmse, Rozanne; Wong, Ho Ning; Smit, Frans J.; Haynes, Richard K.; N'Da, David D. (Wiley, 2017)Dihydroartemisinin (DHA), either used in its own right or as the active drug generated in vivo from the other artemisinins in current clinical use—artemether and artesunate—induces quiescence in ring-stage parasites of ... -
Activities of 11-azaartemisinin and N-sulfonyl derivatives against Neospora caninum and comparative cytotoxicities
Harmse, Rozanne; Wong, Ho Ning; Smit, Frans J.; N'Da, David D.; Haynes, Richard K. (Wiley, 2017)Neosporosis caused by the apicomplexan parasite Neospora caninum is an economically important disease that induces abortion in dairy and beef cattle. There are no vaccines or drugs available on the market for control or ... -
The case for development of 11-aza-artemisinins for malaria
Harmse, Rozanne; Smit, Frans; Haynes, Richard K.; N'Da, David D.; Wong, Ho Ning (Bentham Science, 2015)The current treatment regimens for uncomplicated malaria comprise an artemisinin in combination with another drug (ACT). However, the recent emergence of resistance to ACTs in South East Asia dramatically emphasizes the ... -
Design, synthesis, and antimycobacterial activity of novel ciprofloxacin derivatives
Cilliers, Pieter; Smit, Frans J.; Aucamp, Janine; N'Da, David D.; Seldon, Ronnett (Wiley, 2019)Tuberculosis is the deadliest infectious disease affecting humankind with a death toll of approximately 1.7 million people in 2016. The increasing prevalence of multidrug‐resistant strains of the causative pathogen, ... -
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 ... -
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 ... -
Single-step synthesis and in vitro anti-mycobacterial activity of novel nitrofurantoin analogues
Zuma, Nonkululeko H.; Smit, Frans J.; Aucamp, Janine; N'Da, David D.; Seldon, Ronnett (Elsevier, 2020)The emergence of drug-resistant tuberculosis (DR-TB) as well as the requirement for long, expensive and toxic drug regimens impede efforts to control and eliminate TB. Therefore, there’s a need for effective and affordable ... -
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 antimycobacterial activity of disubstituted benzyltriazoles
Smit, Frans J.; Aucamp, Janine; N'Da, David D.; Seldon, Ronnett; Jordaan, Audrey (Springer, 2019)The increasing prevalence of multidrug-resistant strains of Mycobacterium tuberculosis (Mtb), the pathogen of human tuberculosis (TB), serves as a strong incentive for the discovery and development of new agents for the ... -
Synthesis and biological evaluation of a series of non-hemiacetal ester derivatives of artemisinin
Zuma, Nonkululeko H.; Smit, Frans J.; N'Da, David D.; De Kock, Carmen; Combrinck, Jill (Elsevier, 2016)In an attempt to improve the efficacy and stability of current, clinically used artemisinins, a series non-hemiacetal ester derivatives of artemisinin were synthesized and evaluated for their in vitro antiplasmodial and ... -
Synthesis and in vitro antimycobacterial and antileishmanial activities of hydroquinone-triazole hybrids
Horn, Chris-Marie; Aucamp, Janine; Smit, Frans J.; N'Da, David D.; Seldon, Ronnett (Springer, 2020)Infectious diseases such as tuberculosis and leishmaniasis are leading causes of human death. One of the major factors contributing to the poor control of these diseases is primarily the reduced effectiveness of the existing ... -
Synthesis and in vitro biological activities of ferrocenyl-chalcone amides
Smit, Frans J.; Bezuidenhout, Jaco J.; Bezuidenhout, Carlos C.; N'Da, David D. (Springer, 2016)A series of aminoferrocenyl–chalcone amides 11–19 were synthesized through condensation of a carboxylic acid-functionalized chalcone 10 with ferrocenylamines, using 1,1′-carbonyldiimidazole as the coupling agent. The ... -
Synthesis and in vitro biological evaluation of aminoacridines and artemisinin-acridine hybrids
Joubert, Juan P.; Smit, Frans J.; Du Plessis, Lissinda; N'Da, David D.; Smith, Peter J. (Elsevier, 2014)During this study, 9-aminoacridine and artemisinin–acridine hybrid compounds were synthesized and the in vitro for antimalarial activity against both the chloroquine sensitive but also gametocytocidal strain (NF54), and ... -
Synthesis and in vitro biological evaluation of dihydroartemisinyl-chalcone esters
Smit, Frans J.; N'Da, David D.; Van Biljon, Riëtte A.; Birkholtz, Lyn-Marie (Elsevier, 2015)A series of dihydroartemisinyl-chalcone esters were synthesized through esterification of chalcones with dihydroartemisinin (DHA). The hybrids were screened against chloroquine (CQ) sensitive (3D7) and CQ resistant (W2) ... -
Synthesis, antimalarial activities and cytotoxicities of amino-artemisinin-1,2-disubstituted ferrocene hybrids
De Lange, Christo; Smit, Frans J.; Wentzel, Johannes F.; Wong, Ho Ning; Haynes, Richard K.; N'Da, David D. (Elsevier, 2018)Artemisinin-ferrocene conjugates incorporating a 1,2-disubstituted ferrocene analogous to that embedded in ferroquine but attached via a piperazine linker to C10 of the artemisinin were prepared from the piperazine artemisinin ... -
Synthesis, in vitro antimalarial activities and cytotoxicities of amino-artemisinin-ferrocene derivatives
De Lange, Christo; Smit, Frans J.; Wentzel, Johannes F.; Wong, Ho Ning; Haynes, Richard K.; N'Da, David D. (Elsevier, 2018)Novel derivatives bearing a ferrocene attached via a piperazine linker to C-10 of the artemisinin nucleus were prepared from dihydroartemisinin and screened against chloroquine (CQ) sensitive NF54 and CQ resistant K1 and ... -
Synthesis, in vitro antimalarial activity and cytotoxicity of novel 4-aminoquinolinyl-chalcone amides
Smit, Frans J.; N'Da, David D. (Elsevier, 2014)A series of 4-aminoquinolinyl-chalcone amides 11–19 were synthesized through condensation of carboxylic acid-functionalized chalcone with aminoquinolines, using 1,10-carbonyldiimidazole as coupling agent. These compounds ...