The scientists: With the emergence of strains of Plasmodium falciparum that are developing resistance against the currently most effective antimalarial drugs, a new class of antimalarials is urgently required. At the Open Lab, Leena Keurulainen and Mikko Vahermo, doctoral researchers working in a group headed by Dr. Jari Yli-Kauhaluoma, Professor and Head of the Pharmaceutical Chemistry Division and jointly supervised by Dr. Paula Kiuru, a post-doctoral researcher at the University of Helsinki are focusing their research to try to identify and synthesize an antimalarial lead compound with a benzimidazole core.
The sponsor: The University of Helsinki was founded in 1640. It is one of the best multidisciplinary research universities in the world. The high-quality research creates new knowledge for educating specialists in various fields as well as for utilisation in social decision-making and the business sector. The University of Helsinki is an active, international academic community of 40,000 students and staff members. It operates on four campuses in Helsinki and at 17 other locations.
Foundation funding: The Foundation is providing £135,240 in support of this research.
GSK’s contribution: GSK is providing in-kind contributions (including facilities and expertise from supporting scientists for HTS and access to the compounds library).
Project Description: Leena and Mikko are using a benzimidazoIe derivative synthesized at the University of Helsinki which has shown activity against protozoan parasites. Following this discovery, Leena and Mikko conducted a structure search of the Tres Cantos Antimalarial Set (TCAMS) which led to the identification of some structural analogues which are endowed with antiplasmodial properties. At the Open Lab, Leena and Mikko are focusing on the optimization of this series with the ultimate objective of finding a lead with good therapeutic efficacy in the mouse model of Plasmodium falciparum infection that could eventually be further developed.
GSK´s expertise in biological testing and ADMET will greatly improve the speed of the development cycles and this in turn gives our project a bigger chance of being successful. (Leena Keurulainen, Open Lab Scientist)