Browsing Faculty of Health Sciences by Author "N'Da, David D."
Now showing items 1-20 of 42
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1-Bromo-2-(10 β-dihydroartemisinoxy)-ethane
Lombard, Marli C.; N'Da, David D.; Breytenbach, Jaco C.; Fernandes, Manuel A. (IUCr, 2010)The title compound, C17H27BrO5, DEB, is a derivative of artemisinin which is used in malaria therapy. The OR-group at C12 is cis to the CH3-group at C11 and axially oriented on ring D which has a chair conformation. The ... -
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 ... -
Antimalarial and anticancer activities of artemisinin-quinoline hybrid-dimers and pharmacokinetic properties in mice
Lombard, Marli C.; N'Da, David D.; Breytenbach, Jaco C.; Kolesnikova, Natasha I.; Tran van Ba, Christophe (Elsevier, 2012)Malaria, one of the three most important life-threatening infectious diseases, is recommended to be treated with ACT (artemisinin combination therapy) against which Plasmodium falciparum already displayed resistance. Two ... -
Artemisinin quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity
Lombard, Marli C.; N'Da, David D.; Breytenbach, Jaco C.; Smith, Peter J.; Lategan, Carmen A. (Elsevier, 2010)Novel artemisinin–quinoline hybrid-dimers were synthesized from dihydroartemisinin and different aminoquinolines at elevated temperatures (90–110 °C). All compounds were obtained as the β-isomers and were tested against ... -
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 ... -
Cell based assays for anti-Plasmodium activity evaluation
Mokgethi-Morule, Thabang; N'Da, David D. (Elsevier, 2016)Malaria remains one of the most common and deadly infectious diseases worldwide. The severity of this global public health challenge is reflected by the approximately 198 million people, who were reportedly infected in ... -
Effects of oral administration of synthesized d-amides of eflornithine in the rat
Helena, Kevin J.; N'Da, David D.; Breytenbach, Jaco C.; Ashton, Michael; Johansson, Carl (Thieme, 2010)The purpose of this study was to synthesize a series of δ-amide derivatives of the antitrypanosomal drug eflornithine (2,5-diamino-2-(difluoromethyl)pentanoic acid hydrochloride, DMFO, CAS 70052-12-9), to determine their ... -
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes
Aucamp, Janine; Zuma, Nonkululeko H.; N'Da, David D. (Elsevier, 2020)Leishmaniasis is a neglected tropical disease affecting thousands worldwide, especially in developing countries where it co-exists with malaria. Only a handful of drugs are clinically available to treat the disease, but ... -
In-vitro transdermal penetration of cytarabine and its N4-alkylamide derivatives
Legoabe, Lesetja J.; Breytenbach, Jaco C.; N'Da, David D.; Breytenbach, J. Wilma (Wiley, 2010)Objectives The aim of this study was to synthesise and determine the transdermal penetration of cytarabine alkylamide derivatives and assess the correlation of flux with physicochemical properties. Methods The alkylamide ... -
Inhibitory effects of novel ciprofloxacin derivatives on the growth of four Babesia species and Theileria equi
Batiha, Gaber El-Saber; N'Da, David D.; Dickson, Stuart Tayebwa; Beshbishy, Amany Magdy; Yokoyama, Naoaki (Springer, 2020)The problems of parasite resistance, as well as the toxic residues to most of the commercially available antipiroplasmic drugs severely weaken their effective, curative, and environmental safe employment. Therefore, it is ... -
Mono-, di- and trisubstituted derivatives of eflornithine: synthesis for in vivo delivery of DL-alpha-difluoromethylornithine in plasma
Cloete, Theunis T.; N'Da, David D.; Breytenbach, Jaco C.; Johansson, Carl C.; Kumar Vodnala, Suman (Thieme, 2011)The aim of this study was to synthesize a series of mono-, di- and trisubstituted derivatives of the human African trypanosomiasis drug eflornithine (alpha-difluoromethylornithine, DMFO, CAS 70052-12-9) to determine their ... -
Prodrug strategies for enhancing the percutaneous absorption of drugs
N'Da, David D. (MDPI, 2014)The transdermal application of drugs has attracted increasing interest over the last decade or so, due to the advantages it offers, compared to other delivery methods. The development of an efficient means of transdermal ... -
Recent advances in the synthesis and development of nitroaromatics as anti-infective drugs
Kannigadu, Christina; N'Da, David D. (Bentham Science, 2020)Infectious diseases commonly occur in tropical and sub-tropical countries. The pathogens of such diseases are able to multiply in human hosts, warranting their continual survival. Infections that are commonplace include ... -
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 antimalarial activity of ethylene glycol oligomeric ethers of artemisinin
Steyn, Minette; N'Da, David D.; Breytenbach, Jaco C.; Breytenbach, Wilma J.; Smith, Peter J.; Meredith, Sandra (Wiley, 2011)Objectives The aim of this study was to synthesize a series of ethylene glycol ether derivatives of the antimalarial drug artemisinin, determine their values for selected physicochemical properties and evaluate their ... -
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 ...