Promising Compounds for Development of Malaria Drug

Using a high-throughput screening (HTS) assay, British investigators have identified three compounds that are structurally related and that kill blood-stage malaria parasites. Widespread resistance to current drugs has created an urgent need for effective new anti-malaria compounds.

Researchers from the Assay Development Group at Medical Research Council Technology and the MRC National Institute for Medical Research (NIMR, London, UK) had a hit rate of 0.66% after screening 10,000 randomly selected compounds drawn from the compound library of Maybridge plc (Tintagel, UK). They used a novel fluorescence-based high-throughput screening assay that utilized a synthetic peptide substrate for a recombinant malaria protease. Hits showed good selectivity for the target protease when tested against a range of mammalian and bacterial serine proteases.

"We believe that these compounds are a good starting point for anti-malarial drug discovery,” said Dr. Michael Dalrymple, director of applied research at MRCT. "This project is a tripartite interaction between MRC scientists, Maybridge plc, and MRCT.”

Maybridge is a leading producer of organic compounds used in HTS and combinatorial chemistry. Its HTS collection consists of more than 53,000 organic drug-like compounds produced by innovative synthetic techniques.





Related Links:
MRC National Inst.
Maybridge