There were ~219 million cases of malaria and 660,000 deaths in 2010, while an estimated 3.3 billion people were at risk of malaria in 2011. The treatment and control of malaria is increasingly difficult due to the spread of resistance to antimalarial drugs. Artemisinin-based combination therapies (ACTs) are currently the first-line of treatment, however resistance to multiple ACTs has already emerged, leading to concern about their long-term viability. In order to continue successful treatment and ultimate eradication of malaria it is essential to develop new medicines with novel modes of action.
Work at Leeds has identified a main and back-up chemical series which are extremely potent in enzyme assay and blood cultures. We worked with the group to develop project proposals to generate the robust data required for an application to an external translational drug discovery scheme. These applications were successfully submitted to University funding schemes which support the translation of biomedical research, and the financial support was augmented with Sector Hub proof-of-concept funding. The projects have explored the structure-activity relationship to identify compounds with improved metabolic stability and selectivity while retaining their potency. This has allowed the group to develop applications for external translational funding.