3 research outputs found
Detection of telomerase activity in Plasmodium falciparum using a nonradioactive method
Screening of a library of traditional Chinese medicines to identify anti-malarial compounds and extracts
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery
Most malaria drug development focuses on parasite stages detected in red blood cells, even though to achieve eradication, next-generation drugs active against both erythrocytic and exo-erythrocytic forms would be preferable. We applied a multifactorial approach to a set of 1 microM), and identified chemical scaffolds with potent activity against both forms. From this screen, we identified an imidazolopiperazine scaffold series that was highly enriched among compounds active against Plasmodium liver stages. Our orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 mg/kg) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity. The open source chemical tools resulting from our effort provide starting points for future drug discovery programs, as well as opportunities for researchers to investigate the biology of exo-erythrocytic form