An Endoperoxide-Based Hybrid Approach to Deliver Falcipain Inhibitors Inside Malaria Parasites (pages 1528–1536)
Rudi Oliveira, Ana S. Newton, Dr. Rita C. Guedes, Daniela Miranda, Dr. Richard K. Amewu, Dr. Abhishek Srivastava, Dr. Jiri Gut, Prof. Philip J. Rosenthal, Prof. Paul M. O'Neill, Prof. Stephen A. Ward, Dr. Francisca Lopes and Prof. Rui Moreira
Article first published online: 12 JUL 2013 | DOI: 10.1002/cmdc.201300202
Parasite fighters: A series of tetraoxane–vinyl sulfone hybrids generate toxic radicals once activated inside malaria parasites, releasing highly active falcipain-2 (FP-2) inhibitors in situ. These hybrids are active within the low nanomolar range against chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum strains and may present alternatives to current antimalarial chemotherapeutics.