Short synthesis and antimalarial activity of fagaronine.

Abstract

Herein, we report a new synthesis of fagaronine 1, inspired by the synthesis reported by Luo for nornitidine. The in vitro biological activity of fagaronine against malaria on several chloroquine-sensitive and resistant Plasmodium falciparum strains was confirmed, and the selectivity index compared to mammalian cells was calculated. Fagaronine was found to have very good antimalarial activity in vivo, comparable to the activity of the reference compound chloroquine. Therefore, fagaronine appears to be a good potential lead for the design of new antimalarial molecules.

• Authors: M Rivaud, A Mendoza, M Sauvain, A Valentin, V Jullian
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 20 Issue 15 Pg. 4856-61 (Aug 01 2012) ISSN: 1464-3391 [Electronic] England
• PMID: 22766218 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier Ltd. All rights reserved.

Chemical References

• Antimalarials
• Benzophenanthridines
• fagaronine
• Chloroquine

Topics

• Animals
• Antimalarials (chemical synthesis, chemistry, pharmacology)
• Benzophenanthridines (chemical synthesis, chemistry, pharmacology)
• Chlorocebus aethiops
• Chloroquine (pharmacology)
• Disease Models, Animal
• Dose-Response Relationship, Drug
• Drug Resistance (drug effects)
• Female
• Mice
• Molecular Structure
• Parasitic Sensitivity Tests
• Plasmodium falciparum (drug effects)
• Structure-Activity Relationship
• Vero Cells