TC045

Identifying benzimidazole-derived leads against P falciparum

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Principal Investigator (PI)

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Project location

the sponsor

Home Institution

The University of Helsinki

foundation funding

Foundation funding

The Foundation is providing £135,240 in support.

Open Labs Fellow/s

Leena Keurulainen - Mikko Vahermo

GSK’s contribution

GSK provides in-kind contributions (including facilities and expertise from supporting scientists for HTS and access to the compounds library).

Project Description

Leena and Mikko used 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)