Ontology highlight
ABSTRACT:
SUBMITTER: Vial HJ
PROVIDER: S-EPMC523447 | biostudies-literature | 2004 Oct
REPOSITORIES: biostudies-literature
Vial Henri J HJ Wein Sharon S Farenc Christine C Kocken Clemens C Nicolas Olivier O Ancelin Marie Laure ML Bressolle Francoise F Thomas Alan A Calas Michèle M
Proceedings of the National Academy of Sciences of the United States of America 20041018 43
We created neutral antimalarial prodrugs that deliver bisthiazolium compounds with antimalarial activity in the nanomolar range. These drugs primarily affect early intraerythrocytic stages through rapid, nonreversible cytotoxicity. The compounds are suitable for both parenteral and oral use and plasma promotes rapid conversion of the prodrug into the drug. We demonstrate that very low doses offer protection in a murine model of malaria. The drugs show great potential for curing high parasitemia ...[more]