1. Evaluation of substituted phenalenone analogues as antiplasmodial agents
- Author
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Teresa Abad-Grillo, David Gutiérrez, Grant McNaughton-Smith, and Ninoska Flores
- Subjects
Erythrocytes ,biology ,Stereochemistry ,Immunology ,Plasmodium falciparum ,Chloroquine ,General Medicine ,Phenalenes ,biology.organism_classification ,Antimalarials ,Inhibitory Concentration 50 ,Infectious Diseases ,parasitic diseases ,medicine ,Humans ,Parasitology ,Structural motif ,medicine.drug - Abstract
A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiplasmodial activities against a strain of chloroquine sensitive Plasmodium falciparum F32. Two compounds exhibited considerable effects against the malaria parasite (IC50 ⩽ 1 μg/mL), one of which maintained the same level of activity in a chloroquine-resistant strain. This is the first record of antiplasmodial activity on this type of scaffold, providing a new structural motif as a new lead for antimalarial activity.
- Published
- 2012