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Synthesis and biomimetic chemistry of novel antimalarial endoperoxide cysteine protease inhibitor (ECPI) pro-drugs
Reference
B13581
Principal Investigator / Supervisor
Prof. Paul ONeill
Co-Investigators /
Co-Supervisors
Professor Stephen Ward
Institution
University of Liverpool
Department
Chemistry
Funding type
Research
Value (£)
175,224
Status
Completed
Type
Research Grant
Start date
01/09/2000
End date
01/09/2003
Duration
36 months
Abstract
Licochalcone A and other chalcone analogues have been shown to be potent antimalarial cysteine protease inhibitors. Based on this knowledge, and on a sound mechanistic understanding of the biomimetic Fe (II) catalysed degradation of the endoperoxide drug arteflene, we now wish to prepare a series of endoperoxide cysteine protease inhibitor (ECPI) pro-drugs that will selectively deliver the protease inhibitor to its site of action by ferrous catalysed unmasking in the malarial parasite food vacuole. This represents a new approach to antimalarial drug design in that in addition to the intraparasitic generation of the biologically active cysteine protease inhibitor, endoperoxide cleavage will also release cytotoxic C-centred radicals.
Summary
unavailable
Committee
Closed Committee - Biomolecular Sciences (BMS)
Research Topics
X – not assigned to a current Research Topic
Research Priority
X – Research Priority information not available
Research Initiative
X - not in an Initiative
Funding Scheme
X – not Funded via a specific Funding Scheme
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