New dual-acting antimalarial compounds discovered

Novartis and MMV have identified a new class of compounds that targets both the blood- and liver-stage infections of malaria

17 Nov 2011

The discovery of a new class of dual-acting antimalarial compounds – the imidazolopiperazines (IZPs) – was published in the journal Science online, on the Science Express website today. The findings report on compounds that target both liver and blood infections, attacking the Plasmodium parasite at both stages in its reproduction cycle.
 
The findings describe how MMV, Novartis and other partners developed a novel assay to determine liver-stage activity of candidate small molecules, then used the assay and other tools to identify and optimize a chemical scaffold with activity on both blood- and liver-stage parasites in malaria mouse models. Several other compound classes, also with dual activity, are described and released by Novartis through ChEMBL – Neglected Tropical Disease at www.ebi.ac.uk/chemblntd.
 
“MMV has been collaborating with Novartis, the Dutch Primate Centre, Swiss Tropical and Public Health Institute and the Wellcome Trust on this exciting project for almost 4 years now,” said Tim Wells, CSO, Medicines for Malaria Venture. “Preventing the infection in the liver is an important part of preventing infections in the community. The potential of this class of compounds to prevent transmission of the disease is one of the key attributes we need in new drugs targeting malaria eradication.”