Margaret A. L. Blackie

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To establish the role of the ferrocenyl moiety in the antiplasmodial activity of ferroquine, compounds in which this moiety is replaced by the corresponding ruthenium-based moieties were synthesized and evaluated. In both the sensitive (D10) and resistant (K1) strains of Plasmodium falciparum, ruthenoquine analogues showed comparable potency to ferroquine.(More)
Over the last decade, a significant body of research has been developed around the inclusion of a metallocene moiety into known antimalarial compounds. Ferroquine is the most successful of these compounds. Herein, we describe our contribution to metallocene antimalarials. Our approach has sought to introduce diversity sites in the side chain of ferroquine(More)
Synthesis of the potent antiplasmodial 4-aminoquinoline, phenylequine (PQ), is reported for the first time. PQ and the two analogues show increased efficacy in moving from the chloroquine sensitive D10 to the chloroquine resistant K1 strain in vitro. The in vivo efficacy of PQ, and salts thereof, have been determined in Plasmodium berghei ANKA and(More)
Research into metal complexes of known antimalarial drugs have been known for 30 years. Initial exploration into this field was fairly slow and largely limited to the synthesis of the complexes and reporting of antiplasmodial efficacy. In the last five years this approach has shifted substantially. Increasingly papers dealing with the mechanism of action,(More)
With the emergence of resistance to artemesinin, the need for new antimalarial compounds is pressing. Several research groups have made significant contributions to the exploration of the use of 1,2,4,5-tetraoxanes and 1,2,4- trioxanes as synthetic analogues of artemesinin. This short review highlights the recent developments in this field detailing both(More)
Malaria continues to affect millions of people annually. With the rise of drug resistant strains, the need for alternative treatments has become increasingly urgent. Recently, PfUCHL3 was identified as an essential deubiquitinating enzyme. The increasing number of drug target structures being solved has increased the feasibility of utilizing a structural(More)
The synthesis and in vitro evaluation of novel triazole-linked chloroquinoline derivatives as potential antiplasmodial agents against Plasmodium falciparum is reported. The 15 synthesized target compounds were obtained by means of a copper(I)-mediated click reaction between a variety of 1,2- and 1,3-azidoamines and(More)
Using 2,8-bis(trifluoromethyl)quinoline, the pharmacophore of mefloquine, as scaffold, eleven novel triazole-linked compounds have been synthesised by the application of CuAAC chemistry. The in vitro biological activity of the compounds on the Plasmodium falciparum chloroquine-sensitive strain NF54 was then determined. The compounds all showed IC50s in the(More)
7-Chloroquinoline-based antimalarial drugs are effective in the inhibition of hemozoin formation in the food vacuole of the Plasmodium parasite, the causative agent of malaria. We synthesized five series of ferroquine (FQ) and phenylequine (PQ) derivatives, which display good in vitro efficacy toward both the chloroquine-sensitive (CQS) NF54 (IC50 : 4.2 nm)(More)
Potential drug molecules are often discarded due to poor physicochemical properties and pharmacokinetic profiles. As such, research into the use of multicomponent crystal systems (such as salts and co-crystals) is currently being conducted with the aim of improving the properties of the molecule, without altering the bioactivity of the drug. Although(More)