Alasdair Hill

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Following a program undertaken to identify hit compounds against NADH:ubiquinone oxidoreductase (PfNDH2), a novel enzyme target within the malaria parasite Plasmodium falciparum, hit to lead optimization led to identification of CK-2-68, a molecule suitable for further development. In order to reduce ClogP and improve solubility of CK-2-68 incorporation of(More)
A program was undertaken to identify hit compounds against NADH:ubiquinone oxidoreductase (PfNDH2), a dehydrogenase of the mitochondrial electron transport chain of the malaria parasite Plasmodium falciparum. PfNDH2 has only one known inhibitor, hydroxy-2-dodecyl-4-(1H)-quinolone (HDQ), and this was used along with a range of chemoinformatics methods in the(More)
Malaria is responsible for approximately 1 million deaths annually; thus, continued efforts to discover new antimalarials are required. A HTS screen was established to identify novel inhibitors of the parasite's mitochondrial enzyme NADH:quinone oxidoreductase (PfNDH2). On the basis of only one known inhibitor of this enzyme, the challenge was to discover(More)
A novel drug for uncomplicated malaria: targeted high throughput screening (HTS) against the type II NADH:ubiquinone oxidoreductase (PfNdh2) of Plasmodium falciparum Steve A Ward, Nicholas Fisher, Alasdair Hill, Alison Mbekeani, Alison Shone, Gemma Nixon, Paul Stocks, Peter Gibbons, Richard Amewu, David W Hong, Victoria Barton, Chandra Pidathala, James(More)
The semisynthetic artemisinin derivatives such as artesunate and artemether, along with the fully synthetic endoperoxide antimalarials (e.g., OZ277, Nature 2004, 430, 900-904), are believed to mediate their antimalarial effects by iron-induced formation of carbon-centered radicals capable of alkylating heme and/or protein. Here, we describe the design and(More)
Development of a novel drug for uncomplicated malaria targeting the mitochondrial NADH: quinone oxidoreductase Giancarlo A Biagini, Alasdair Hill, Alison Mbekeani, Alison Shone, Gemma Nixon, Paul Stocks, Peter Gibbons, Richard Amewu, David W Hong, Victoria Barton, Chandra Pidathala, James Chadwick, Louise Le Pensee, Ashley Warman, Raman Sharma, Nick Fisher,(More)
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