|Phenotypic whole cell high-throughput screening has identified the 2-aminopyridines as a class of small molecules with promising antimalarial activity . From this series, UCT943 was optimized for antiplasmodial activity by structural modification of the clinical candidate MMV048 and shown to have asexual blood stage, transmission-blocking, and liver stage activities [1-2]. UCT943 was being developed as a back-up compound to MMV048 but has been withdrawn due to preclinical toxicity concerns.
The compound formulation is claimed in patent WO2013121387 .
Potential Target/Mechanism Of Action: Genomic experiments provide evidence that the molecular target of UCT943 is the Plasmodium lipid kinase, phosphatidylinositol 4-kinase (PfPI4K) . This lipid kinase has been proposed to act at the Golgi to regulate essential membrane trafficking events .