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The evaluation of metal co-ordinating bis-thiosemicarbazones as potential anti-malarial agents
(Bentham Science, 2019)
Background:
The emergence of resistance to the artemisinins which are the current mainstays for antimalarial chemotheraphy has created an environment where the development of new drugs acting in a mechanistally discrete ...
Preliminary evaluation of artemisinin-cholesterol conjugates as potential drugs for the treatment of intractable forms of malaria and tuberculosis
(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 ...
Optimal 10-aminoartemisinins with potent transmission-blocking capabilities for new artemisinin combination therapies-activities against blood stage P. falciparum including PfKI3 C580Y mutants and liver stage P. berghei parasites
(Frontiers, 2020)
We have demonstrated previously that amino-artemisinins including artemiside and artemisone in which an amino group replaces the oxygen-bearing substituents attached to C-10 of the current clinical artemisinin derivatives ...
In vitro efficacy of synthesized artemisinin derivatives against Leishmania promastigotes
(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 ...
Anti-trypanosomal and antimalarial properties of tetralone derivatives and structurally related benzocycloalkanones
(MDPI, 2019)
Background and objectives: Sleeping sickness and malaria alike are insect-borne protozoan
diseases that share overlapping endemic areas in sub-Saharan Africa. The causative agent for malaria
has developed resistance ...
Artemisia afra, a controversial herbal remedy or a treasure trove of new drugs?
(Elsevier, 2019)
Ethnoparmacological relevance
Artemisia afra is one of the most widely used herbal remedies in South Africa. This highly aromatic shrub is used to treat various disorders including coughs, colds, influenza, and malaria. ...
Evaluation and optimization of synthetic routes from dihydroartemisinin to the alkylamino-artemisinins artemiside and artemisone: a test of N-glycosylation methodologies on a lipophilic peroxide
(Elsevier, 2018)
10-Alkylamino-artemisinins including artemiside and artemisone display enhanced activities against malaria. Earlier, dihydroartemisinin (DHA) TMS ether was converted by trimethylsilyl bromide into the 10-β-bromide that ...
Development of pyridyl thiosemicarbazones as highly potent agents for the treatment of malaria after oral administration
(Oxford Univ Press, 2019)
Objectives
Drug resistance exists to all current and investigational antimalarial drug classes. Consequently, we have set out to develop chemically and mechanistically discrete antimalarials. Here we report on the development ...
Antimalarial and anticancer activities of artemisinin-quinoline hybrid-dimers and pharmacokinetic properties in mice
(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 ...
Absorption of the novel artemisinin derivatives artemisone and artemiside: potential application of Pheroid™ technology
(Elsevier, 2011)
Artemisinins have low aqueous solubility that results in poor and erratic absorption upon oral administration. The poor solubility and erratic absorption usually translate to low bioavailability. Artemisinin-based monotherapy ...